Custom and Pre-Selected Kinase Profilingto fit your Budget and Needs!

As of April 12, 2024

128
Tyrosine
Kinases

197

Serine/Threonine
Kinases

27

Lipid
Kinases

Carna Biosciences, Inc.
2007 Carna Biosciences, Inc.

Profiling Assays available from Carna Biosciences, Inc.
As of April 12, 2024

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Kinase Name
ABL(ABL1)
ABL(ABL1)[E255K]
ABL(ABL1)[T315I]
ACK(TNK2)
AKT1
AKT2
AKT3
ALK
ALK[C1156Y]
ALK[F1174L]
ALK[G1202R]
ALK[G1269A]
ALK[L1196M]
ALK[R1275Q]
ALK[T1151_L1152insT]
EML4-ALK
NPM1-ALKAMPKα1/β1/γ1(PRKAA1/B1/G1)
AMPKα2/β1/γ1(PRKAA2/B1/G1)
ARG(ABL2)
AurA(AURKA)
AurA(AURKA)/TPX2
AurB(AURKB)/INCENP
AurC(AURKC)
AXL
BLK
BMX
BRK(PTK6)
BRSK1
BRSK2
BTK
BTK[C481S]
BUB1/BUB3
CaMK1α(CAMK1)
CaMK1δ(CAMK1D)
CaMK2α(CAMK2A)
CaMK2β(CAMK2B)
CaMK2γ(CAMK2G)
CaMK2δ(CAMK2D)
CaMK4
CDC7/ASK
CDK1(CDC2)/CycB1
CDK2/CycA2
CDK2/CycE1
CDK3/CycE1
CDK4/CycD3
CDK5/p25
CDK6/CycD3
CDK7/CycH/MAT1
CDK9/CycT1
CGK2(PRKG2)
CHK1(CHEK1)
CHK2(CHEK2)
CK1α(CSNK1A1)
CK1γ1(CSNK1G1)
CK1γ2(CSNK1G2)
CK1γ3(CSNK1G3)
CK1δ(CSNK1D)
CK1ε(CSNK1E)
CK2α1/β(CSNK2A1/B)
CK2α2/β(CSNK2A2/B)
CLK1
CLK2
CLK3
CRIK(CIT)CSKDAPK1DCAMKL2
DDR1
DDR2
DGKα(DGKA)
DGKβ(DGKB)
DGKγ(DGKG)
DGKδ(DGKD)
DGKε(DGKE)
DGKζ(DGKZ)
DGKη(DGKH)
DGKθ(DGKQ)
DGKι(DGKI)
DGKκ(DGKK)DYRK1ADYRK1B
DYRK2
DYRK3
EEF2K

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37
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38
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38

Assay Platform

MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
MSA
MSA
MSA
MSA
MSA

2

Kinase Name
EGFR
EGFR[C797S/L858R]
EGFR[d746-750]
EGFR[d746-750/C797S]
EGFR[d746-750/T790M]
EGFR[d746-750/T790M/C797S]
EGFR[D770_N771insNPG]
EGFR[L858R]
EGFR[L861Q]
EGFR[T790M]
EGFR[T790M/C797S/L858R]
EGFR[T790M/L858R]
EPHA1
EPHA2
EPHA3
EPHA4
EPHA5
EPHA6
EPHA7
EPHA8
EPHB1
EPHB2
EPHB3
EPHB4
Erk1(MAPK3)
Erk2(MAPK1)
Erk5(MAPK7)FAK(PTK2)
FER
FES
FGFR1
FGFR1[V561M]
FGFR2
FGFR2[V564I]
FGFR3
FGFR3[K650E]
FGFR3[K650M]
FGFR3[V555L]
FGFR3[V555M]
FGFR4
FGFR4[N535K]
FGFR4[V550E]
FGFR4[V550L]
FGR
FLT1
FLT3
FLT4
FMS(CSF1R)
FRK
FYN[isoform a]
FYN[isoform b]
GSK3α(GSK3A)
GSK3β(GSK3B)
Haspin(GSG2)
HCK
HER2(ERBB2)
HER4(ERBB4)
HGK(MAP4K4)
HIPK1
HIPK2
HIPK3
HIPK4
HPK1(MAP4K1)
IGF1R
IKKα(CHUK)IKKβ(IKBKB)IKKε(IKBKE)
INSR
IRAK1
IRAK4
IRR(INSRR)
ITK
JAK1
JAK2
JAK3
JNK1(MAPK8)JNK2(MAPK9)JNK3(MAPK10)KDRKITKIT[D816E]
KIT[D816V]
KIT[D816Y]
KIT[T670I]
KIT[V560G]

Assay Platform

MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
IMAP
MSA
MSA
MSA
IMAP
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA

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Kinase NameKIT[V654A]
LATS1/MOBKL1A
LATS2/MOBKL1ALCKLOK(STK10)
LTK
LYNa
LYNb
MAP4K2
MAPKAPK2
MAPKAPK3
MAPKAPK5
MARK1
MARK2
MARK3
MARK4
MELK
MER(MERTK)
MET
MET[D1228H]
MET[M1250T]
MET[Y1235D]
MINK(MINK1)
MNK1(MKNK1)
MNK2(MKNK2)MRCKα(CDC42BPA)MRCKβ(CDC42BPB)
MSK1(RPS6KA5)
MSK2(RPS6KA4)MSSK1(STK23)
MST1(STK4)
MST2(STK3)
MST3(STK24)
MST4
MUSK
NDR1(STK38)
NDR2(STK38L)
NEK1
NEK2
NEK4
NEK6
NEK7
NEK9
NIM1K(MGC42105)
NuaK1
NuaK2
p38α(MAPK14)p38β(MAPK11)p38γ(MAPK12)p38δ(MAPK13)
p70S6K(RPS6KB1)
p70S6Kβ(RPS6KB2)
PAK1
PAK2
PAK4
PAK5(PAK7)
PAK6
PASK
PBK
PDGFRα(PDGFRA)PDGFRα(PDGFRA)[D842V]
PDGFRα(PDGFRA)[T674I]PDGFRα(PDGFRA)[V561D]PDGFRβ(PDGFRB)PDHK2(PDK2)
PDHK4(PDK4)
PDK1(PDPK1)PEK(EIF2AK3)
PGK(PRKG1)
PHKG1
PHKG2
PIK3CA/PIK3R1
PIK3CA[E542K]/PIK3R1
PIK3CA[E545K]/PIK3R1
PIK3CA[H1047R]/PIK3R1
PIK3CA[P539R]/PIK3R1
PIK3CA[R88Q]/PIK3R1
PIK3CB/PIK3R1
PIK3CD/PIK3R1
PIKFYVE(PIP5K3)
PIM1
PIM2
PIM3
PIP4K2A
PIP4K2B
PIP5K1A
PIP5K1B
PIP5K1C
PIP5KL1
PKACα(PRKACA)

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Assay Platform

MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
IMAP
MSA
MSA
MSA
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
MSA
MSA
MSA
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
ADP-Glo
MSA

3Kinase NamePKACβ(PRKACB)PKACγ(PRKACG)
PKCα(PRKCA)
PKCβ1(PRKCB1)
PKCβ2(PRKCB2)
PKCγ(PRKCG)
PKCδ(PRKCD)PKCε(PRKCE)
PKCζ(PRKCZ)
PKCη(PRKCH)
PKCθ(PRKCQ)PKCι(PRKCI)
PKD1(PRKD1)
PKD2(PRKD2)
PKD3(PRKD3)PKN1
PKR(EIF2AK2)
PLK1
PLK2
PLK3
PRKX
PYK2(PTK2B)
QIK(SNF1LK2)RET
RET[G691S]
RET[M918T]
RET[S891A]
RET[Y791F]
ROCK1
ROCK2
RON(MST1R)
ROS(ROS1)
RSK1(RPS6KA1)
RSK2(RPS6KA3)
RSK3(RPS6KA2)
RSK4(RPS6KA6)
SGK
SGK2
SGK3(SGKL)SIK(SNF1LK)
skMLCK(MYLK2)
SLK
SPHK1
SPHK2
SRC
SRM(SRMS)
SRPK1
SRPK2
SYK
TAK1-TAB1(MAP3K7)
TAOK2
TBK1
TEC
TIE2(TEK)TNIKTNK1TRKA(NTRK1)
TRKB(NTRK2)
TRKC(NTRK3)
TSSK1
TSSK2
TSSK3
TXK
TYK2
TYRO3
WNK1
WNK2
WNK3
YES(YES1)YES(YES1)[T348I]
ZAP70

Assay Platform

MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
IMAP
IMAP
MSA
IMAP
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
ADP-Glo
ADP-Glo
MSA
MSA
IMAP
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA

<< Cascade Assay >>Page

Kinase Name

Assay Platform

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72
72
72
72
73
73
73
73
73
74
74
74
74
74
75
75
75
75
75
76

BRAF
BRAF[V600E]
COT(MAP3K8)
DLK(MAP3K12)
MAP2K1
MAP2K2
MAP2K3
MAP2K4
MAP2K5
MAP2K6
MAP2K7
MAP3K1
MAP3K2
MAP3K3
MAP3K4
MAP3K5
MLK1(MAP3K9)
MLK2(MAP3K10)
MLK3(MAP3K11)
MOS
RAF1

MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA
MSA

4

ABL(ABL1)

Assay platform
Substrate

Product code: 08-001
Full-length human ABL [2-1130(end) amino acids of accession
number NP_005148.2] was expressed as N-terminal His-tagged
protein (126 kDa) using baculovirus expression system.

ABL(ABL1)[E255K]

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 75
IC50 at 1 mM ATP (nM) : 1300

Assay platform
Substrate

Product code: 08-094
Full-length human ABL [2-1130(end) amino acids and E255K ofaccession number NP_005148.2] was expressed as N-terminal Histagged protein (126 kDa) using baculovirus expression system.

ABL(ABL1)[T315I]
Full-length human ABL [2-1130(end) amino acids and T315I ofaccession number NP_005148.2] was expressed as N-terminal Histagged protein (126 kDa) using baculovirus expression system.

ACK(TNK2)
Human ACK, catalytic domain [110-476 amino acids of accession
number NP_005772.3] was expressed as N-terminal GST-fusion
protein (69 kDa) using baculovirus expression system.

AKT1

: MSA
: WASP peptide

ATP (μM) Km app / Bin : 97 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.2
IC50 at 1 mM ATP (nM) : 3.8

Assay platform
Substrate

Product code: 01-101: MSA: ABLtide

ATP (μM) Km app / Bin : 4 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 6.4
IC50 at 1 mM ATP (nM) : 890

Assay platform
Substrate

Product code: 08-196: MSA: ABLtide

ATP (μM) Km app / Bin : 17 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 140
IC50 at 1 mM ATP (nM) : 4500

Assay platform
Substrate

Product code: 08-093: MSA: ABLtide: MSA: Crosstide

Human AKT1, catalytic domain [104-480(end) amino acids and
G478S of accession number NP_005154.2] was co-expressed as N- ATP (μM) Km app / Bin : 31 / 50
terminal GST-fusion protein (70 kDa) with His-tagged PDK1 [1Metal: Mg
556(end) amino acids of accession number NP_002604.1] using
Reference compound : Staurosporine
baculovirus expression system.

IC50 at ATP Bin (nM)
: 2.7
IC50 at 1 mM ATP (nM) : 22

5

AKT2

Assay platform
Substrate

Product code: 01-102
Human AKT2, catalytic domain [120-481(end) amino acids ofaccession number NP_001617.1] was co-expressed as N-terminal
GST-fusion protein (69 kDa) with His-tagged PDK1 [1-556(end)amino acids of accession number NP_002604.1] using baculovirus
expression system.

AKT3

ATP (μM) Km app / Bin : 110 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 5.2
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-103
Human AKT3, catalytic domain [108-479(end) amino acids ofaccession number NP_005456.1] was co-expressed as N-terminal
GST-fusion protein (70 kDa) with His-tagged PDK1 [1-556(end)amino acids of accession numberNP_002604.1] using baculovirus
expression system.

ALK
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and I1461V, K1491R, D1529E of accession number NP_004295.2]
was expressed as N-terminal GST-fusion protein (90 kDa) using
baculovirus expression system.

ALK[C1156Y]
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and C1156Y, I1461V, K1491R, D1529E of accession number
NP_004295.2] was expressed as N-terminal GST-fusion protein (90kDa) using baculovirus expression system.

ALK[F1174L]
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and F1174L, I1461V, K1491R, D1529E of accession number
NP_004295.2] was expressed as N-terminal GST-fusion protein (90kDa) using baculovirus expression system.

6

: MSA
: Srctide

ATP (μM) Km app / Bin : 64 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.9
IC50 at 1 mM ATP (nM) : 11

Assay platform
Substrate

Product code: 08-519: MSA: Srctide

ATP (μM) Km app / Bin : 57 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.5
IC50 at 1 mM ATP (nM) : 15

Assay platform
Substrate

Product code: 08-530: MSA: Crosstide

ATP (μM) Km app / Bin : 54 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.2
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-518: MSA: Crosstide: MSA: Srctide

ATP (μM) Km app / Bin : 49 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.4
IC50 at 1 mM ATP (nM) : 21

ALK[G1202R]

Assay platform
Substrate

Product code: 08-544
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and G1202R, I1461V, K1491R, D1529E of accession number
NP_004295.2] was expressed as N-terminal GST-fusion protein (90kDa) using baculovirus expression system.

ALK[G1269A]

ATP (μM) Km app / Bin : 31 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 7.3
IC50 at 1 mM ATP (nM) : 69

Assay platform
Substrate

Product code: 08-537
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and G1269A, I1461V, K1491R, D1529E of accession number
NP_004295.2] was expressed as N-terminal GST-fusion protein (90kDa) using baculovirus expression system.

ALK[L1196M]
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and L1196M, I1461V, K1491R, D1529E of accession number
NP_004295.2] was expressed as N-terminal GST-fusion protein (90kDa) using baculovirus expression system.

ALK[R1275Q]
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and R1275Q, I1461V, K1491R, D1529E of accession number
NP_004295.2] was expressed as N-terminal GST-fusion protein (90kDa) using baculovirus expression system.

ALK[T1151_L1152insT]
Human ALK , cytoplasmic domain [1058-1620(end) amino acids
and T1151_L1152insT, I1461V, K1491R, D1529E of accession
number NP_004295.2] was expressed as N-terminal GST-fusion
protein (90 kDa) using baculovirus expression system.

7

: MSA
: Srctide

ATP (μM) Km app / Bin : 84 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.3
IC50 at 1 mM ATP (nM) : 16

Assay platform
Substrate

Product code: 08-539: MSA: Srctide

ATP (μM) Km app / Bin : 57 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.66
IC50 at 1 mM ATP (nM) : 4.3

Assay platform
Substrate

Product code: 08-520: MSA: Srctide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.36
IC50 at 1 mM ATP (nM) : 1.6

Assay platform
Substrate

Product code: 08-529: MSA: Srctide: MSA: Srctide

ATP (μM) Km app / Bin : 110 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 6.5
IC50 at 1 mM ATP (nM) : 16

EML4-ALK

Assay platform
Substrate

Product code: 08-516
Fused gene of human fusion EML4-ALK [1-1059 amino acids ofaccession number BAF73611.1] was expressed as N-terminal GSTfusion protein (145 kDa) using baculovirus expression system.

NPM1-ALK

ATP (μM) Km app / Bin : 43 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.9
IC50 at 1 mM ATP (nM) : 16

Assay platform
Substrate

Product code: 08-517
Fused gene of human fusion NPM1-ALK [1-680 amino acids ofaccession number BAA08343.1] was expressed as N-terminal GSTfusion protein (103kDa) using baculovirus expression system.

AMPKα1/β1/γ1(PRKAA1/B1/G1)
Full-length human AMPKα1 [1-550(end) amino acids of accession
number NP_006242.4] was co-expressed as N-terminal GST-fusion
protein (90 kDa) with GST-PRKAB1 [1-270(end) amino acids ofaccession number NP_006244.2] and PRKAG1 [1-331(end) aminoacids of accession number NP_002724.1] using baculovirus
expression system. GST-AMPKα1/β1/γ1 was purified by using
glutathione sepharose chromatography and activated with Histagged CaMKK1. Activated GST-AMPKα1/β1/γ1 was purified byusing glutathione sepharose chromatography.

AMPKα2/β1/γ1(PRKAA2/B1/G1)
Full-length human AMPKα2 [1-552(end) amino acids of accession
number NP_006243.2] was co-expressed as N-terminal GST-fusion
protein (89 kDa) with GST-PRKAB1 [1-270(end) amino acids ofaccession number NP_006244.2] and PRKAG1 [1-331(end) aminoacids of accession number NP_002724.1] using baculovirus
expression system. GST-AMPKα2/β1/γ1 was purified by using
glutathione sepharose chromatography and activated with Histagged CaMKK1. Activated GST-AMPKα2/β1/γ1 was purified byusing glutathione sepharose chromatography.

ARG(ABL2)
Full-length human ARG [2-1161(end) amino acids of accession
number NP_001161708.1] was expressed as N-terminal GSTfusion protein (153 kDa) using baculovirus expression system.

8

: MSA
: SAMS peptide

ATP (μM) Km app / Bin : 100 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.79IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-102: MSA: SAMS peptide

ATP (μM) Km app / Bin : 130 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.41
IC50 at 1 mM ATP (nM) : 0.87

Assay platform
Substrate

Product code: 02-114: MSA: Srctide

ATP (μM) Km app / Bin : 57 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.4
IC50 at 1 mM ATP (nM) : 14

Assay platform
Substrate

Product code: 02-113: MSA: Srctide: MSA: ABLtide

ATP (μM) Km app / Bin : 24 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 27
IC50 at 1 mM ATP (nM) : 400

AurA(AURKA)

Assay platform
Substrate

Product code: 05-101
Full-length human AurA [1-403(end) amino acids of accession
number NP_940835.1] was expressed as N-terminal GST-fusion
protein (73 kDa) using baculovirus expression system.

AurA(AURKA)/TPX2

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.8
IC50 at 1 mM ATP (nM) : 17

Assay platform
Substrate

Product code: 05-101
Full-length human AurA [1-403(end) amino acids of accession
number NP_940835.1] was expressed as N-terminal GST-fusion
protein (73 kDa) using baculovirus expression system.

AurB(AURKB)/INCENP
Full-length human AurB [1-344(end) amino acids and M298T ofaccession number NP_004208.2] was co-expressed as N-terminal
GST-fusion protein (66 kDa) with His-tagged INCENP(INBOX) [803918(end) amino acids of accession number NP_001035784.1]
using baculovirus expression system.

AurC(AURKC)
Full-length human AurC [1-275(end) amino acids of accession
number NP_003151.2] was expressed as N-terminal GST-fusion
protein (59 kDa) using baculovirus expression system.

AXL
Human AXL, cytoplasmic domain [464-885(end) amino acids ofaccession number NP_001690.2] was expressed as N-terminal
GST-fusion protein (74 kDa) using baculovirus expression system.

9

: MSA
: Kemptide

ATP (μM) Km app / Bin : 24 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.1
IC50 at 1 mM ATP (nM) : 18

Assay platform
Substrate

Product code: 08-107: MSA: Kemptide

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 7.1
IC50 at 1 mM ATP (nM) : 62

Assay platform
Substrate

Product code: 05-103: MSA: Kemptide

ATP (μM) Km app / Bin : 1.7 / 2
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 6.1
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-102: MSA: Kemptide: MSA: CSKtide

ATP (μM) Km app / Bin : 32 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.1
IC50 at 1 mM ATP (nM) : 7.9

BLK

Assay platform
Substrate

Product code: 08-164
Full-length human BLK [1-505(end) amino acids of accession
number NP_001706.2] was expressed as N-terminal GST-fusion
protein (85 kDa) using baculovirus expression system.

BMX

ATP (μM) Km app / Bin : 62 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.6
IC50 at 1 mM ATP (nM) : 17

Assay platform
Substrate

Product code: 08-179
Full-length human BMX [1-675(end) amino acids of accession
number NP_001712.1] was expressed as N-terminal GST-fusion
protein (105 kDa) using baculovirus expression system.

BRK(PTK6)
Full-length human BRK [2-451(end) amino acids of accession
number NP_005966.1] was expressed as N-terminal GST-fusion
protein (79 kDa) using baculovirus expression system.

BRSK1
Full-length human BRSK1 [1-778(end) amino acids of accession
number NP_115806.1] was expressed as N-terminal GST-fusion
protein (112 kDa) using baculovirus expression system.

BRSK2
Full-length human BRSK2 [1-674(end) amino acids of accession
number ABA17261.1] was expressed as N-terminal GST-fusion
protein (102 kDa) using baculovirus expression system.

10

: MSA
: CHKtide

ATP (μM) Km app / Bin : 30 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.27
IC50 at 1 mM ATP (nM) : 0.57

Assay platform
Substrate

Product code: 02-116: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 250 / 250
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 260
IC50 at 1 mM ATP (nM) : 390

Assay platform
Substrate

Product code: 02-115: MSA: Srctide

ATP (μM) Km app / Bin : 75 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 10
IC50 at 1 mM ATP (nM) : 45

Assay platform
Substrate

Product code: 08-165: MSA: Srctide: MSA: CHKtide

ATP (μM) Km app / Bin : 31 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.31
IC50 at 1 mM ATP (nM) : n.a.

BTK

Assay platform
Substrate

Product code: 08-180
Full-length human BTK [2-659(end) amino acids of accession
number NP_000052.1] was expressed as N-terminal GST-fusion
protein (103 kDa) using baculovirus expression system.

BTK[C481S]

ATP (μM) Km app / Bin : 22 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 24
IC50 at 1 mM ATP (nM) : 93

Assay platform
Substrate

Product code: 08-547
Full-length human BTK [2-659(end) amino acids and C481S ofaccession number NP_000052.1] was expressed as N-terminal
GST-fusion protein (103 kDa) using baculovirus expression system.

BUB1/BUB3
Full-length human BUB1 [1-1085(end) amino acids of accession
number NP_004327] was co-expressed as N-terminal GST-fusion
protein (149 kDa) with DYKDDDDK tagged BUB3 [1-328 (end)amino acids of accession number NP_004716] using baculovirus
expression system.

CaMK1α(CAMK1)
Full-length human CaMK1α [1-370(end) amino acids of accession
number NP_003647.1] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

CaMK1δ(CAMK1D)
Full-length human CaMK1δ[1-357(end) amino acid of accession
number NP_065130.1] was expressed as N-terminal GST-fusion
protein (67 kDa) using baculovirus expression system.

11

: MSA
: GS peptide

ATP (μM) Km app / Bin : 750 / 1000
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 16
IC50 at 1 mM ATP (nM) : 16

Assay platform
Substrate

Product code: 02-106: MSA: H2A peptide

ATP (μM) Km app / Bin : 2.9 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 300
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-104: MSA: Srctide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 37
IC50 at 1 mM ATP (nM) : 170

Assay platform
Substrate

Product code: 05-187: MSA: Srctide: MSA: Synapsin peptide

ATP (μM) Km app / Bin : 11 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.5
IC50 at 1 mM ATP (nM) : n.a.

CaMK2α(CAMK2A)

Assay platform
Substrate

Product code: 02-109
Full-length human CaMK2α [1-478(end) amino acids of accession
number NP_741960.1] was expressed as N-terminal GST-fusion
protein (81 kDa) using baculovirus expression system.

CaMK2β(CAMK2B)

ATP (μM) Km app / Bin : 33 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.75
IC50 at 1 mM ATP (nM) : 3.2

Assay platform
Substrate

Product code: 02-110
Full-length human CaMK2β [1-503 amino acids of accession
number NP_742078.1] was expressed as N-terminal GST-fusion
protein (83 kDa) using baculovirus expression system.

CaMK2γ(CAMK2G)
Full-length human CaMK2γ[1-518(end) amino acids of accession
number NP_751910.1] was expressed as N-terminal GST-fusion
protein (85 kDa) using baculovirus expression system.

CaMK2δ(CAMK2D)
Full-length human CaMK2δ [1-478 amino acids of accession
number NP_742113.1] was expressed as N-terminal GST-fusion
protein (81 kDa) using baculovirus expression system.

CaMK4Full-length human CaMK4 [1-473(end) amino acids of accession
number NP_001735.1] was expressed as N-terminal GST-fusion
protein (79 kDa) using baculovirus expression system.

12

: MSA
: GS peptide

ATP (μM) Km app / Bin : 6.3 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.26
IC50 at 1 mM ATP (nM) : 0.64

Assay platform
Substrate

Product code: 02-108: MSA: GS peptide

ATP (μM) Km app / Bin : 23 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.39IC50 at 1 mM ATP (nM) : 1.1

Assay platform
Substrate

Product code: 02-111: MSA: GS peptide

ATP (μM) Km app / Bin : 19 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.54
IC50 at 1 mM ATP (nM) : 5.8

Assay platform
Substrate

Product code: 02-112: MSA: GS peptide: MSA: GS peptide

ATP (μM) Km app / Bin : 20 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 140
IC50 at 1 mM ATP (nM) : 1000

CDC7/ASK

Assay platform
Substrate

Product code: 05-109
Full-length human CDC7 [1-574(end) amino acids of accession
number NP_003494.1] was co-expressed as N-terminal GST-fusion
protein (92 kDa) with Dbf4(ASK) [1-674(end) amino acids ofaccession number NP_006707.1] using baculovirus expression
system.

CDK1(CDC2)/CycB1

ATP (μM) Km app / Bin : 2.8 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 16
IC50 at 1 mM ATP (nM) : 1600

Assay platform
Substrate

Product code: 04-102
Full-length human CDK1 [1-297(end) amino acids of accession
number NP_001777.1] was co-expressed as N-terminal GST-fusion
protein (61 kDa) with CyclinB1 [1-433(end) amino acids ofaccession number NP_114172.1] using baculovirus expression
system.

CDK2/CycA2
Full-length human CDK2 [1-298(end) amino acids of accession
number NP_001789.2] was co-expressed as N-terminal GSTtagged protein (61 kDa) with GST-CyclinA2 [1-432(end) aminoacids of accession number NP_001228.1] using baculovirus
expression system.

CDK2/CycE1
Full-length human CDK2 [1-298(end) amino acids of accession
number NP_001789.2] was co-expressed as N-terminal GSTtagged protein (61 kDa) with CyclinE1 [1-410(end) amino acids ofaccession number NP_001229.1] using baculovirus expression
system.

CDK3/CycE1
Full-length human CDK3 [1-305(end) amino acids of accession
number NP_001249.1] was co-expressed as N-terminal GST-fusion
protein (62kDa) with CyclinE1 [1-410(end) amino acids ofaccession number NP_001229.1] using baculovirus expression
system.

13: MSA: Modified Histone H1

ATP (μM) Km app / Bin : 130 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.8
IC50 at 1 mM ATP (nM) : 10

Assay platform
Substrate

Product code: 04-104: MSA: Modified Histone H1

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 7.1

Assay platform
Substrate

Product code: 04-165: MSA: Modified Histone H1

ATP (μM) Km app / Bin : 34 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.3
IC50 at 1 mM ATP (nM) : 32

Assay platform
Substrate

Product code: 04-103: MSA: MCM2 peptide: MSA: Modified Histone H1

ATP (μM) Km app / Bin : 1000 / 1000
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.4
IC50 at 1 mM ATP (nM) : 3.4

CDK4/CycD3

Assay platform
Substrate

Product code: 04-105
Full-length human CDK4 [1-303(end) amino acids of accession
number NP_000066.1] was co-expressed as N-terminal GST-fusion
protein (61 kDa) with human GST-CyclinD3 [1-292(end) aminoacids and S259A of accession number NP_001751.1] using
baculovirus expression system.

CDK5/p25

ATP (μM) Km app / Bin : 200 / 200
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 13
IC50 at 1 mM ATP (nM) : 52

Assay platform
Substrate

Product code: 04-106
Full-length human CDK5 [1-292(end) amino acids of accession
number NP_004926.1] was co-expressed as N-terminal GST-fusion
protein (60 kDa) with p25 [99-307(end) amino acids of accession
number NP_003876.1] using baculovirus expression system.

CDK6/CycD3: MSA: DYRKtide-F: MSA: Modified Histone H1

ATP (μM) Km app / Bin : 10 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.5
IC50 at 1 mM ATP (nM) : 86

Product code: 04-107

Assay platform
Substrate

Full-length human CDK6 [1-326(end) amino acids of accession
number NP_001250.1] was co-expressed as N-terminal GST-fusion
protein (64 kDa) with human GST-CyclinD3 [1-292(end) aminoacids and S259A of accession number NP_001751.1] using
baculovirus expression system. GST-CDK6/CycD3 was purified byusing glutathione sepharose chromatography and activated with
His-CDK7/CycH/MAT1. Activated GST-CDK6/CycD3 was purified
using glutathione sepharose chromatography.

ATP (μM) Km app / Bin : 330 / 300
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 58
IC50 at 1 mM ATP (nM) : 110

CDK7/CycH/MAT1

Assay platform
Substrate

Product code: 04-108
Full-length human CDK7 [1-346(end) amino acids of accession
number NP_001790.1] was co-expressed as N-terminal GST-fusion
protein (66 kDa) with CyclinH [1-323(end) amino acids of accession
number NP_001230.1] and MAT1 [1-309(end) amino acids ofaccession number NP_002422.1] using baculovirus expression
system.

CDK9/CycT1
Full-length human CDK9 [1-372(end) amino acids of accession
number NP_001252.1] was co-expressed as N-terminal GST-fusion
protein (70 kDa) with His-CyclinT1 [1-726(end) amino acids ofaccession number NP_001231.2] using baculovirus expression
system.

14: MSA: CTD3 peptide

ATP (μM) Km app / Bin : 32 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 17
IC50 at 1 mM ATP (nM) : 120

Assay platform
Substrate

Product code: 04-110: MSA: DYRKtide-F: MSA: CDK9 substrate

ATP (μM) Km app / Bin : 9.4 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 5.2
IC50 at 1 mM ATP (nM) : 130

CGK2(PRKG2)

Assay platform
Substrate

Product code: 01-143
Full-length human CGK2 [1-762(end) amino acids of accession
number NP_006250.1] was expressed as N-terminal GST-fusion
protein (114 kDa) using baculovirus expression system.

CHK1(CHEK1)

ATP (μM) Km app / Bin : 24 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.88
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-117
Full-length human CHK1 [1-476(end) amino acids and I471V ofaccession number NP_001265.2] was expressed as N-terminal
GST-fusion protein (81 kDa) using baculovirus expression system.

CHK2(CHEK2)
Full-length human CHK2 [1-543(end) amino acids of accession
number NP_009125.1] was expressed as N-terminal GST-fusion
protein (88 kDa) using baculovirus expression system.

CK1α(CSNK1A1)
Full-length human CK1α [1-337(end) amino acids of accession
number NP_001883.4] was expressed as N-terminal GST-fusion
protein (66 kDa) using baculovirus expression system.

CK1γ1(CSNK1G1)
Full-length human CK1γ1 [1-422(end) amino acids of accession
number NP_071331.2] was expressed as N-terminal GST-fusion
protein (76 kDa) using baculovirus expression system.

15

: MSA
: CKtide

ATP (μM) Km app / Bin : 4.1 / 5
Metal
: Mg
Reference compound : 5-Iodotubercidin
IC50 at ATP Bin (nM)
: 150
IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 03-105: MSA: CHKtide

ATP (μM) Km app / Bin : 51 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 11
IC50 at 1 mM ATP (nM) : 25

Assay platform
Substrate

Product code: 03-101: MSA: CHKtide

ATP (μM) Km app / Bin : 50 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.24
IC50 at 1 mM ATP (nM) : 1.1

Assay platform
Substrate

Product code: 02-162: MSA: Kemptide: MSA: CKtide

ATP (μM) Km app / Bin : 6.3 / 5
Metal
: Mg
Reference compound : 5-Iodotubercidin
IC50 at ATP Bin (nM)
: 1300IC50 at 1 mM ATP (nM) : n.a.

CK1γ2(CSNK1G2)

Assay platform
Substrate

Product code: 03-106
Full-length human CK1γ2 [1-415(end) amino acids of accession
number NP_001310.3] was expressed as N-terminal GST-fusion
protein (75 kDa) using baculovirus expression system.

CK1γ3(CSNK1G3)

ATP (μM) Km app / Bin : 10 / 10
Metal
: Mg
Reference compound : 5-Iodotubercidin
IC50 at ATP Bin (nM)
: 510
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 03-107
Full-length human CK1γ3 [1-447(end) amino acids of accession
number NP_004375.2] was expressed as N-terminal GST-fusion
protein (78 kDa) using baculovirus expression system.

CK1δ(CSNK1D)
Human CK1δ, catalytic domain [1-294 amino acids of accession
number NP_001884.2] was expressed as N-terminal GST-fusion
protein (61 kDa) using E. coli expression system.

CK1ε(CSNK1E)
Human CK1ε, catalytic domain [1-348 amino acids of accession
number NP_001885.1] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

CK2α1/β(CSNK2A1/B)
Full-length human CK2α1 [1-391(end) amino acids of accession
number NP_001886.1] was co-expressed as N-terminal GST-fusion
protein (72 kDa) with human His-tagged CK2β [1-215 amino acidsof accession number NP_001311.3] using baculovirus expression
system.

16: MSA: CKtide

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : 5-Iodotubercidin
IC50 at ATP Bin (nM)
: 300
IC50 at 1 mM ATP (nM) : 5800

Assay platform
Substrate

Product code: 05-184: MSA: CKtide

ATP (μM) Km app / Bin : 7.7 / 10
Metal
: Mg
Reference compound : 5-Iodotubercidin
IC50 at ATP Bin (nM)
: 25
IC50 at 1 mM ATP (nM) : 570

Assay platform
Substrate

Product code: 03-104: MSA: CKtide

ATP (μM) Km app / Bin : 3.2 / 5
Metal
: Mg
Reference compound : 5-Iodotubercidin
IC50 at ATP Bin (nM)
: 920
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 03-103: MSA: CKtide: MSA: CK2tide

ATP (μM) Km app / Bin : 2.9 / 5
Metal
: Mg
Reference compound : TBB
IC50 at ATP Bin (nM)
: 60
IC50 at 1 mM ATP (nM) : 4800

CK2α2/β(CSNK2A2/B)

Assay platform
Substrate

Product code: 05-185
Full-length human CK2α2 [1-350(end) amino acids of accession
number NP_001887.1] was co-expressed as N-terminal GST-fusion
protein (68 kDa) with human His-tagged CK2β [1-215 amino acidsof accession number NP_001311.3] using baculovirus expression
system.

CLK1

ATP (μM) Km app / Bin : 2.1 / 5
Metal
: Mg
Reference compound : TBB
IC50 at ATP Bin (nM)
: 50
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 04-126
Human CLK1, catalytic domain [129-484(end) amino acids ofaccession number NP_004062.2] was expressed as N-terminal
GST-fusion protein (69 kDa) using baculovirus expression system.

CLK2
Full-length human CLK2 [1-499(end) amino acids of accession
number NP_001281267.1] was expressed as N-terminal GSTfusion protein (87 kDa) using baculovirus expression system.

CLK3
Full-length human CLK3 [1-490(end) amino acids of accession
number NP_003983.2] was expressed as N-terminal GST-fusion
protein (86 kDa) using baculovirus expression system.

CRIK(CIT)
Human citron kinase (CRIK), catalytic domain [1-449 amino acids ofaccession number NP_009105.1] was expressed as N-terminal
GST fusion protein (77 kDa) using baculovirus expression system.

17

: MSA
: DYRKtide-F

ATP (μM) Km app / Bin : 75 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 820
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-104: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 140 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.6
IC50 at 1 mM ATP (nM) : 28

Assay platform
Substrate

Product code: 04-128: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 11 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 9.6
IC50 at 1 mM ATP (nM) : 60

Assay platform
Substrate

Product code: 04-127: MSA: CK2tide: MSA: Histone H3 peptide

ATP (μM) Km app / Bin : 7.8 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 31
IC50 at 1 mM ATP (nM) : n.a.

CSK

Assay platform
Substrate

Product code: 08-111
Full-length human CSK [1-450(end) amino acids of accession
number NP_004374.1] was expressed as N-terminal GST-fusion
protein (78 kDa) using baculovirus expression system.

DAPK1

ATP (μM) Km app / Bin : 4.8 / 5
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 53
IC50 at 1 mM ATP (nM) : 1500

Assay platform
Substrate

Product code: 02-134
Human DAPK1, catalytic domain [1-289 amino acids of accession
number NP_004929.1] was expressed as N-terminal GST-fusion
protein (60 kDa) using baculovirus expression system.

DCAMKL2
Full-length human DCAMKL2 [1-695(end) amino acids of accession
number NP_689832.1] was expressed as N-terminal GST-fusion
protein (103 kDa) using baculovirus expression system.

DDR1
Human DDR1, cytoplasmic domain [444-876(end) amino acids ofaccession number NP_001945.3] was expressed as N-terminal
GST-fusion protein (75 kDa) using baculovirus expression system.

DDR2
Human DDR2, cytoplasmic domain [422-855(end) amino acids ofaccession number NP_006173.2] was expressed as N-terminal
GST-fusion protein (77 kDa) using baculovirus expression system.

18

: MSA
: IRS1

ATP (μM) Km app / Bin : 94 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.0
IC50 at 1 mM ATP (nM) : 3.1

Assay platform
Substrate

Product code: 08-114: MSA: GS peptide

ATP (μM) Km app / Bin : 120 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 22
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-113: MSA: DAPK1tide

ATP (μM) Km app / Bin : 1.1 / 1
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.9
IC50 at 1 mM ATP (nM) : 490

Assay platform
Substrate

Product code: 02-140: MSA: Srctide: MSA: IRS1

ATP (μM) Km app / Bin : 38 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.2
IC50 at 1 mM ATP (nM) : 0.77

DGKα(DGKA)

Assay platform
Substrate

Product code: 12-401-20N
Full-length human DGKα [1-735(end) amino acids of accession
number NP_958852.1] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (87 kDa) using baculovirus expression
system.

DGKβ(DGKB)

ATP (μM) Km app / Bin : 130 / 100
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-402-20N
Full-length human DGKβ [1-803(end) amino acids of accession
number NP_001337638.1] was expressed as N-terminalDYKDDDDK tagged, biotinylated protein (95 kDa) using baculovirus
expression system. The protein was purified by using DYKDDDDK
tag antibody agarose and activated with ATP. Activated protein was
purified by using gel filtration.

DGKγ(DGKG)
Full-length human DGKγ [1-791(end) amino acids and T142S and
R316K of accession number NP_001337.2] was expressed as Nterminal DYKDDDDK tagged, biotinylated protein (94 kDa) using
baculovirus expression system.

DGKδ(DGKD)
Catalytic domain of human DGKδ [1-1141 amino acids of accession
number NP_690618.2] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (131 kDa) using baculovirus expression
system.

DGKε(DGKE)
Truncated human DGKε [48-567(end) amino acids of accession
number NP_003638.1] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (63 kDa) using baculovirus expression
system.

19: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 120 / 100
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-415-20N: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 55 / 50
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-404-20N: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 61 / 50
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-403-20N: ADP-Glo: Diacylglycerol: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 120 / 100
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

DGKζ(DGKZ)Assay platform
Substrate

Product code: 12-410-20N
Full-length human DGKζ [1-929(end) amino acids of accession
number NP_003637.2] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (109 kDa) using baculovirus expression
system.

DGKη(DGKH)

ATP (μM) Km app / Bin : 25 / 25
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-406-20N
Catalytic domain of human DGKη [1-1147 amino acids of accession
number NP_821077.1] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (131 kDa) using baculovirus expression
system.

DGKθ(DGKQ)
Full-length human DGKθ [1-942(end) amino acids of accession
number NP_001338.2] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (106 kDa) using baculovirus expression
system.

DGKι(DGKI)
Full-length human DGKι [1-1065(end) amino acids of accession
number NP_004708.1] was expressed as N-terminal DYKDDDDK
tagged, biotinylated protein (122 kDa) using baculovirus expression
system.

DGKκ(DGKK)
Full-length human DGKκ [1-1271(end) amino acids and D1118N ofaccession number NP_001013764.1] was expressed as N-terminalDYKDDDDK tagged, biotinylated protein (146 kDa) using
baculovirus expression system.

20: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 34 / 50
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-408-20N: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 37 / 50
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-407-20N: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 24 / 25
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 12-409-20N: ADP-Glo: Diacylglycerol: ADP-Glo: Diacylglycerol

ATP (μM) Km app / Bin : 17 / 25
Metal
: Mg
Reference compound : Non-disclosable
IC50 at ATP Bin (nM)
: Non-disclosable
IC50 at 1 mM ATP (nM) : n.a.

DYRK1A

Assay platform
Substrate

Product code: 04-130
Full-length human DYRK1A [1-763(end) amino acids of accession
number NP_001387.2] was expressed as N-terminal GST-fusion
protein (112 kDa) using baculovirus expression system.

DYRK1B

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 7.8
IC50 at 1 mM ATP (nM) : 120

Assay platform
Substrate

Product code: 04-131
Full-length human DYRK1B [1-629(end) amino acids of accession
number NP_004705.1] was expressed as N-terminal GST-fusion
protein (96 kDa) using baculovirus expression system.

DYRK2
Full-length human DYRK2 [1-528(end) amino acids of accession
number NP_003574.1] was expressed as N-terminal GST-fusion
protein (87 kDa) using baculovirus expression system.

DYRK3
Full-length human DYRK3 [1-588(end) amino acids of accession
number NP_003573.2] was expressed as N-terminal GST-fusion
protein (93 kDa) using baculovirus expression system.

EEF2K
Full-length human EEF2K [1-725(end) amino acids of accession
number NP_037434.1] was expressed as N-terminal GST-fusion
protein (109 kDa) using E. coli expression system.

21

: MSA
: DYRKtide-F

ATP (μM) Km app / Bin : 6.8 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 17
IC50 at 1 mM ATP (nM) : 1200

Assay platform
Substrate

Product code: 10-113: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 7.7 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 130
IC50 at 1 mM ATP (nM) : 6300

Assay platform
Substrate

Product code: 04-133: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 59 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.2
IC50 at 1 mM ATP (nM) : 32

Assay platform
Substrate

Product code: 04-132: MSA: DYRKtide-F: MSA: EEF2Ktide

ATP (μM) Km app / Bin : 12 / 10
Metal
: Mg
Reference compound : A-484954
IC50 at ATP Bin (nM)
: 330
IC50 at 1 mM ATP (nM) : n.a.

EGFR

Assay platform
Substrate

Product code: 08-115
Human EGFR, cytoplasmic domain [669-1210(end) amino acids ofaccession number NP_005219.2] was expressed as N-terminal
GST-fusion protein (89 kDa) using baculovirus expression system.

EGFR[C797S/L858R]

ATP (μM) Km app / Bin : 2.7 / 5
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 53
IC50 at 1 mM ATP (nM) : 7700

Assay platform
Substrate

Product code: 08-563
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and C797S/L858R of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (89kDa) using
baculovirus expression system.

EGFR[d746-750]
Human EGFR, cytoplasmic domain [669-745, 751-1210(end) aminoacids of accession number NP_005219.2] was expressed as Nterminal GST-fusion protein (88 kDa) using baculovirus expression
system.

EGFR[d746-750/C797S]
Human EGFR, cytoplasmic domain [669-745, 751-1210(end) aminoacids and C797S of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (88 kDa) using
baculovirus expression system.

EGFR[d746-750/T790M]
Human EGFR, cytoplasmic domain [669-745, 751-1210(end) aminoacids and T790M of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (89 kDa) using
baculovirus expression system.

22

: MSA
: Srctide

ATP (μM) Km app / Bin : 8.2 / 10
Metal
: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 8.0
IC50 at 1 mM ATP (nM) : 130

Assay platform
Substrate

Product code: 08-528: MSA: Srctide

ATP (μM) Km app / Bin : 19 / 25
Metal
: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 13
IC50 at 1 mM ATP (nM) : 93

Assay platform
Substrate

Product code: 08-564: MSA: Srctide

ATP (μM) Km app / Bin : 4.1 / 5
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 8.8
IC50 at 1 mM ATP (nM) : 270

Assay platform
Substrate

Product code: 08-527: MSA: Srctide: MSA: Srctide

ATP (μM) Km app / Bin : 5.4 / 5
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.52
IC50 at 1 mM ATP (nM) : 9.7

EGFR[d746-750/T790M/C797S]

Assay platform
Substrate

Product code: 08-565
Human EGFR, cytoplasmic domain [669-745, 751-1210(end) aminoacids and T790M/C797S of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (88 kDa) using
baculovirus expression system.

EGFR[D770_N771insNPG]

ATP (μM) Km app / Bin : 1.8 / 2
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.84
IC50 at 1 mM ATP (nM) : 14

Assay platform
Substrate

Product code: 08-553
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and D770_N771insNPG of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (89 kDa) using
baculovirus expression system.

EGFR[L858R]
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and L858R of accession number NP_005219.2] was expressed as
N-terminal GST-fusion protein (89 kDa) using baculovirus
expression system.

EGFR[L861Q]
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and L861Q of accession number NP_005219.2] was expressed as
N-terminal GST-fusion protein (89 kDa) using baculovirus
expression system.

EGFR[T790M]
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and T790M of accession number NP_005219.2] was expressed as
N-terminal GST-fusion protein (89 kDa) using baculovirus
expression system.

23

: MSA
: Srctide

ATP (μM) Km app / Bin : 7.5 / 10
Metal
: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 68
IC50 at 1 mM ATP (nM) : 2200

Assay platform
Substrate

Product code: 08-194: MSA: Srctide

ATP (μM) Km app / Bin : 9.8 / 10
Metal
: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 11
IC50 at 1 mM ATP (nM) : 360

Assay platform
Substrate

Product code: 08-513: MSA: Srctide

ATP (μM) Km app / Bin : 2.3 / 5
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 18
IC50 at 1 mM ATP (nM) : 930

Assay platform
Substrate

Product code: 08-502: MSA: Srctide: MSA: Srctide

ATP (μM) Km app / Bin : 0.9 / 1
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.8
IC50 at 1 mM ATP (nM) : 190

EGFR[T790M/C797S/L858R]

Assay platform
Substrate

Product code: 08-559
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and T790M/C797S/L858R of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (89 kDa) using
baculovirus expression system.

EGFR[T790M/L858R]

ATP (μM) Km app / Bin : 0.85 / n.a.
Metal
: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: n.a.
IC50 at 1 mM ATP (nM) : 37

Assay platform
Substrate

Product code: 08-510
Human EGFR, cytoplasmic domain [669-1210(end) amino acids
and T790M/L858R of accession number NP_005219.2] wasexpressed as N-terminal GST-fusion protein (89 kDa) using
baculovirus expression system.

EPHA1
Human EPHA1, cytoplasmic domain [586-976(end) amino acids ofaccession number NP_005223.3] was expressed as N-terminal
GST-fusion protein (71 kDa) using baculovirus expression system.

EPHA2
Human EPHA2, cytoplasmic domain [572-976(end) amino acids ofaccession number NP_004422.2] was expressed as N-terminal
GST-fusion protein (73 kDa) using baculovirus expression system.

EPHA3
Human EPHA3, cytoplasmic domain [579-983(end) amino acids ofaccession number NP_005224.2] was expressed as N-terminal
GST-fusion protein (72 kDa) using baculovirus expression system.

24

: MSA
: Blk/Lyntide

ATP (μM) Km app / Bin : 67 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 160
IC50 at 1 mM ATP (nM) : 530

Assay platform
Substrate

Product code: 08-122: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 22 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 20
IC50 at 1 mM ATP (nM) : 340

Assay platform
Substrate

Product code: 08-121: MSA: Srctide

ATP (μM) Km app / Bin : 1.9 / 2
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 56

Assay platform
Substrate

Product code: 08-119: MSA: Srctide: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 170 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 37
IC50 at 1 mM ATP (nM) : 76

EPHA4

Assay platform
Substrate

Product code: 08-123
Human EPHA4, cytoplasmic domain [586-986(end) amino acids ofaccession number NP_004429.1] was expressed as N-terminal
GST-fusion protein (72 kDa) using baculovirus expression system.

EPHA5

ATP (μM) Km app / Bin : 52 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 50
IC50 at 1 mM ATP (nM) : 330

Assay platform
Substrate

Product code: 08-124
Human EPHA5, catalytic domain [662-948 amino acids ofaccession number NP_004430.3] was expressed as N-terminal
GST-fusion protein (59 kDa) using baculovirus expression system.

EPHA6
Human EPHA6, cytoplasmic domain [683-1130(end) amino acids ofaccession number NP_001073917.2] was expressed as N-terminal
GST-fusion protein (77 kDa) using baculovirus expression system.

EPHA7
Human EPHA7, cytoplasmic domain [595-998(end) amino acids ofaccession number NP_004431.1] was expressed as N-terminal
GST-fusion protein (73 kDa) using baculovirus expression system.

EPHA8
Human EPHA8, catalytic domain [571-924 amino acids ofaccession number NP_065387.1] was expressed as N-terminal
GST-fusion protein (67 kDa) using baculovirus expression system.

25

: MSA
: Blk/Lyntide

ATP (μM) Km app / Bin : 58 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 48
IC50 at 1 mM ATP (nM) : 480

Assay platform
Substrate

Product code: 08-127: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 17
IC50 at 1 mM ATP (nM) : 60

Assay platform
Substrate

Product code: 08-126: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 56 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 34
IC50 at 1 mM ATP (nM) : 220

Assay platform
Substrate

Product code: 08-125: MSA: Blk/Lyntide: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 69 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 61
IC50 at 1 mM ATP (nM) : 240

EPHB1

Assay platform
Substrate

Product code: 08-128
Human EPHB1, cytoplasmic domain [578-984(end) amino acids ofaccession number NP_004432.1] was expressed as N-terminal
GST-fusion protein (73 kDa) using baculovirus expression system.

EPHB2

ATP (μM) Km app / Bin : 29 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 53
IC50 at 1 mM ATP (nM) : 760

Assay platform
Substrate

Product code: 08-129
Human EPHB2, cytoplasmic domain [581-987(end) amino acids ofaccession number NP_004433.2] was expressed as N-terminal
GST-fusion protein (73 kDa) using baculovirus expression system.

EPHB3
Human EPHB3, cytoplasmic domain [596-998(end) amino acids ofaccession number NP_004434.2] was expressed as N-terminal
GST-fusion protein (73 kDa) using baculovirus expression system.

EPHB4
Human EPHB4, cytoplasmic domain [577-987(end) amino acids ofaccession number NP_004435.3] was expressed as N-terminal
GST-protein (73 kDa) using baculovirus expression system.

Erk1(MAPK3)
Full-length human Erk1 [1-379(end) amino acids of accession
number NP_002737.1] was expressed as N-terminal GST-fusion
protein (70 kDa) using E.coli expression system. GST-Erk1 was
purified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K1. Activated GST-Erk1 was
purified using glutathione sepharose chromatography.

26

: MSA
: Blk/Lyntide

ATP (μM) Km app / Bin : 56 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 230
IC50 at 1 mM ATP (nM) : 1500

Assay platform
Substrate

Product code: 04-142: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 49 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2000IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 08-131: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 86 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 73
IC50 at 1 mM ATP (nM) : 400

Assay platform
Substrate

Product code: 08-130: MSA: Blk/Lyntide: MSA: Modified Erktide

ATP (μM) Km app / Bin : 34 / 50
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 37
IC50 at 1 mM ATP (nM) : 400

Erk2(MAPK1)

Assay platform
Substrate

Product code: 04-143
Full-length human Erk2 [1-360(end) amino acids of accession
number NP_002736.3] was expressed as N-terminal GST-fusion
protein (69 kDa) using E.coli expression system. GST-Erk2 waspurified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K1. Activated GST-Erk2 waspurified using glutathione sepharose chromatography.

Erk5(MAPK7)

ATP (μM) Km app / Bin : 33 / 50
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 21
IC50 at 1 mM ATP (nM) : 180

Assay platform
Substrate

Product code: 04-146
Human Erk5, catalytic domain [1-398 amino acids of accession
number NP_002740.2] was expressed as N-terminal GST-fusion
protein (72 kDa) using E. coli expression system. GST-Erk5 was
purified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K5. Activated GST-Erk5 was
purified by using Ni-NTA affinity chromatography.

FAK(PTK2)
Truncated human FAK[376-1052(end) amino acids of accession
number NP_722560.1] was expressed as N-terminal GST-fusion
protein (103 kDa) using baculovirus expression system.

FER
Full-length human FER [1-822(end) amino acids of accession
number NP_005237.1] was expressed as N-terminal GST-fusion
protein (122 kDa) using baculovirus expression system.

FES
Full-length human FES [1-413, 416-822(end) amino acids ofaccession number NP_001996.1] was expressed as N-terminal
GST-fusion protein (120 kDa) using baculovirus expression system.

27

: MSA
: Srctide

ATP (μM) Km app / Bin : 26 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 12

Assay platform
Substrate

Product code: 08-140: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 25 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 47
IC50 at 1 mM ATP (nM) : 230

Assay platform
Substrate

Product code: 08-139: MSA: EGFR-derived peptide

ATP (μM) Km app / Bin : 450 / 1000
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 280
IC50 at 1 mM ATP (nM) : 280

Assay platform
Substrate

Product code: 08-137: MSA: Modified Erktide: MSA: Srctide

ATP (μM) Km app / Bin : 43 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.9
IC50 at 1 mM ATP (nM) : 25

FGFR1

Assay platform
Substrate

Product code: 08-133
Human FGFR1, cytoplasmic domain [398-822(end) amino acids ofaccession number NP_075598.2] was expressed as N-terminal
GST-fusion protein (75 kDa) using baculovirus expression system.

FGFR1[V561M]

ATP (μM) Km app / Bin : 89 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.3
IC50 at 1 mM ATP (nM) : 12

Assay platform
Substrate

Product code: 08-536
Human FGFR1, cytoplasmic domain [398-822(end) amino acids
and V561M of accession number NP_075598.2] was expressed as
N-terminal GST-fusion protein (75 kDa) using baculovirus
expression system.

FGFR2
Human FGFR2, cytoplasmic domain [399-821(end) amino acids ofaccession number NP_000132.3] was expressed as N-terminal
GST-fusion protein (75 kDa) using baculovirus expression system.

FGFR2[V564I]: MSA: CSKtide

ATP (μM) Km app / Bin : 66 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.4
IC50 at 1 mM ATP (nM) : 5.4

Assay platform
Substrate

Product code: 08-546: MSA: CSKtide

ATP (μM) Km app / Bin : 33 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.14
IC50 at 1 mM ATP (nM) : 1.3

Assay platform
Substrate

Product code: 08-134: MSA: CSKtide: MSA: CSKtide

Human FGFR2, cytoplasmic domain [399-821(end) amino acids
and V564I of accession number NP_000132.3] was expressed as N- ATP (μM) Km app / Bin : 21 / 25
terminal GST-fusion protein (75 kDa) using baculovirus expression
Metal
: Mg
system.

Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.0IC50 at 1 mM ATP (nM) : 47

FGFR3

Assay platform
Substrate

Product code: 08-135
Human FGFR3, cytoplasmic domain [436-806(end) amino acids ofaccession number NP_000133.1] was expressed as N-terminal
GST-fusion protein (68 kDa) using baculovirus expression system.

28

: MSA
: CSKtide

ATP (μM) Km app / Bin : 43 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.6
IC50 at 1 mM ATP (nM) : 15

FGFR3[K650E]

Assay platform
Substrate

Product code: 08-501
Human FGFR3, cytoplasmic domain [436-806(end) amino acids
and K650E of accession number NP_000133.1] was expressed as
N-terminal GST-fusion protein (68 kDa) using baculovirus
expression system.

FGFR3[K650M]

ATP (μM) Km app / Bin : 41 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.2
IC50 at 1 mM ATP (nM) : 14

Assay platform
Substrate

Product code: 08-199
Human FGFR3, cytoplasmic domain [436-806(end) amino acids
and K650M of accession number NP_000133.1] was expressed as
N-terminal GST-fusion protein (68 kDa) using baculovirus
expression system.

FGFR3[V555L]
Human FGFR3, cytoplasmic domain [436-806(end) amino acids
and V555L of accession number NP_000133.1] was expressed as
N-terminal GST-fusion protein (68 kDa) using baculovirus
expression system.

FGFR3[V555M]
Human FGFR3, cytoplasmic domain [436-806(end) amino acids
and V555M of accession number NP_000133.1] was expressed as
N-terminal GST-fusion protein (68 kDa) using baculovirus
expression system.

FGFR4
Human FGFR4, cytoplasmic domain [460-802(end) amino acids ofaccession number NP_002002.3] was expressed as N-terminal
GST-fusion protein (65 kDa) using baculovirus expression system.

29

: MSA
: CSKtide

ATP (μM) Km app / Bin : 37 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.21
IC50 at 1 mM ATP (nM) : 1.8

Assay platform
Substrate

Product code: 08-136: MSA: CSKtide

ATP (μM) Km app / Bin : 29 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.49IC50 at 1 mM ATP (nM) : 9.4

Assay platform
Substrate

Product code: 08-543: MSA: CSKtide

ATP (μM) Km app / Bin : 17 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.68
IC50 at 1 mM ATP (nM) : 17

Assay platform
Substrate

Product code: 08-548: MSA: CSKtide: MSA: CSKtide

ATP (μM) Km app / Bin : 230 / 250
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 43
IC50 at 1 mM ATP (nM) : 120

FGFR4[N535K]

Assay platform
Substrate

Product code: 08-524
Human FGFR4, cytoplasmic domain [460-802(end) amino acids
and N535K of accession number NP_002002.3] was expressed as
N-terminal GST-fusion protein (65 kDa) using baculovirus
expression system.

FGFR4[V550E]

ATP (μM) Km app / Bin : 30 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 160
IC50 at 1 mM ATP (nM) : 1200

Assay platform
Substrate

Product code: 08-525
Human FGFR4, cytoplasmic domain [460-802(end) amino acids
and V550E of accession number NP_002002.3] was expressed as
N-terminal GST-fusion protein (65 kDa) using baculovirus
expression system.

FGFR4[V550L]
Human FGFR4, cytoplasmic domain [460-802(end) amino acids
and V550L of accession number NP_002002.3] was expressed as
N-terminal GST-fusion protein (65 kDa) using baculovirus
expression system.

FGR
Full-length human FGR [1-529(end) amino acids of accession
number NP_005239.1] was expressed as N-terminal GST-fusion
protein (86 kDa) using baculovirus expression system.

FLT1
Human FLT1, cytoplasmic domain [781-1338(end) amino acids ofaccession number NP_002010.1] was expressed as N-terminal
GST-fusion protein (90 kDa) using baculovirus expression system.

30

: MSA
: Srctide

ATP (μM) Km app / Bin : 34 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.3
IC50 at 1 mM ATP (nM) : 16

Assay platform
Substrate

Product code: 08-189: MSA: CSKtide

ATP (μM) Km app / Bin : 160 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 10
IC50 at 1 mM ATP (nM) : 44

Assay platform
Substrate

Product code: 08-166: MSA: CSKtide

ATP (μM) Km app / Bin : 210 / 200
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 370
IC50 at 1 mM ATP (nM) : 1300

Assay platform
Substrate

Product code: 08-526: MSA: CSKtide: MSA: CSKtide

ATP (μM) Km app / Bin : 140 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.2
IC50 at 1 mM ATP (nM) : 6.8

FLT3

Assay platform
Substrate

Product code: 08-154
Human FLT3, cytoplasmic domain [564-993(end) amino acids ofaccession number NP_004110.2] was expressed as N-terminal
GST-fusion protein (77 kDa) using baculovirus expression system.

FLT4

ATP (μM) Km app / Bin : 94 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.20IC50 at 1 mM ATP (nM) : 0.34

Assay platform
Substrate

Product code: 08-190
Human FLT4, cytoplasmic domain [798-1298(end) amino acids ofaccession number NP_002011.1] was expressed as N-terminal
GST-fusion protein (83 kDa) using baculovirus expression system.

FMS(CSF1R)
Human FMS, cytoplasmic domain [538-972(end) amino acids ofaccession number NP_005202.2] was expressed as N-terminal
GST-fusion protein (76 kDa) using baculovirus expression system.

FRK
Human FRK, catalytic domain [223-505(end) amino acids ofaccession number NP_002022.1] was expressed as N-terminal
GST-fusion protein (60 kDa) using baculovirus expression system.

FYN[isoform a]
Full-length human FYN [isoform a] [1-537(end) amino acids ofaccession number NP_002028.1] was expressed as N-terminal
GST-fusion protein (88 kDa) using baculovirus expression system.

31

: MSA
: Srctide

ATP (μM) Km app / Bin : 62 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.4
IC50 at 1 mM ATP (nM) : 40

Assay platform
Substrate

Product code: 08-168: MSA: Srctide

ATP (μM) Km app / Bin : 26 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.26
IC50 at 1 mM ATP (nM) : 0.70

Assay platform
Substrate

Product code: 08-167: MSA: CSKtide

ATP (μM) Km app / Bin : 72 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.66
IC50 at 1 mM ATP (nM) : 2.4

Assay platform
Substrate

Product code: 08-155: MSA: Srctide: MSA: Srctide

ATP (μM) Km app / Bin : 36 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.9
IC50 at 1 mM ATP (nM) : 24

FYN[isoform b]

Assay platform
Substrate

Product code: 08-531
Full-length human FYN [isoform b] [1-534(end) amino acids ofaccession number NP_694592.1] was expressed as N-terminal
GST-fusion protein (87 kDa) using baculovirus expression system.

GSK3α(GSK3A)

ATP (μM) Km app / Bin : 20 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.8
IC50 at 1 mM ATP (nM) : 42

Assay platform
Substrate

Product code: 04-140
Full-length human GSK3α [1-483(end) amino acids of accession
number NP_063937.2] was expressed as N-terminal GST-fusion
protein (78 kDa) using baculovirus expression system.

GSK3β(GSK3B)
Full-length human GSK3β [1-420(end) amino acids of accession
number NP_001139628.1] was expressed as N-terminal GSTfusion protein (74 kDa) using baculovirus expression system.

Haspin(GSG2)
Full-length human Haspin [1-798(end) amino acids of accession
number NP_114171.2] was expressed as N-terminal GST-fusion
protein (116 kDa) using baculovirus expression system.

HCK
Truncated human HCK [25-526(end) amino acids of accession
number NP_002101.2] was expressed as N-terminal GST-fusion
protein (84 kDa) using baculovirus expression system.

32

: MSA
: Histone H3 peptide

ATP (μM) Km app / Bin : 140 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 5.8
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-169: MSA: CREBtide-p

ATP (μM) Km app / Bin : 9.1 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 9.2
IC50 at 1 mM ATP (nM) : 240

Assay platform
Substrate

Product code: 05-111: MSA: CREBtide-p

ATP (μM) Km app / Bin : 12 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 15
IC50 at 1 mM ATP (nM) : 400

Assay platform
Substrate

Product code: 04-141: MSA: Srctide: MSA: Srctide

ATP (μM) Km app / Bin : 11 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.1
IC50 at 1 mM ATP (nM) : 22

HER2(ERBB2)

Assay platform
Substrate

Product code: 08-016
Human HER2, cytoplasmic domain [676-1255(end) amino acids
and P1170A of accession number NP_004439.2] was expressed as
N-terminal His-tagged protein (67 kDa) using baculovirus
expression system.

HER4(ERBB4)

ATP (μM) Km app / Bin : 3.5 / 5
Metal
: Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 90
IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 08-118
Human HER4, cytoplasmic domain [676-1308(end) amino acids ofaccession number NP_005226.1] was expressed as N-terminal
GST-fusion protein (99 kDa) using baculovirus expression system.

HGK(MAP4K4)
Human HGK, catalytic domain [1-328 amino acids of accession
number NP_004825.2] was expressed as N-terminal GST-fusion
protein (64 kDa) using baculovirus expression system.

HIPK1
Human HIPK1, catalytic domain [158-555 amino acids of accession
number NP_689909.2] was expressed as N-terminal GST-fusion
protein (73 kDa) using baculovirus expression system.

HIPK2
Full-length human HIPK2 [1-1198(end) amino acids of accession
number NP_073577.3] was expressed as N-terminal GST-fusion
protein (158 kDa) using baculovirus expression system.

33

: MSA
: DYRKtide-F

ATP (μM) Km app / Bin : 4.4 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 570
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 04-136: MSA: Moesin-derived peptide

ATP (μM) Km app / Bin : 9.4 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 23

Assay platform
Substrate

Product code: 04-135: MSA: Srctide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 34
IC50 at 1 mM ATP (nM) : 1000

Assay platform
Substrate

Product code: 07-137: MSA: Srctide: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 5.9 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 170
IC50 at 1 mM ATP (nM) : n.a.

HIPK3

Assay platform
Substrate

Product code: 04-137
Human HIPK3, catalytic domain [161-562 amino acids of accession
number NP_005725.3] was expressed as N-terminal GST-fusion
protein (73 kDa) using baculovirus expression system.

HIPK4

ATP (μM) Km app / Bin : 7.3 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 120
IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 04-138
Full-length human HIPK4 [1-616(end) amino acids of accession
number NP_653286.2] was expressed as N-terminal GST-fusion
protein (96 kDa) using baculovirus expression system.

HPK1(MAP4K1)
Human HPK1, catalytic domain [1-346 amino acids of accession
number NP_009112.1] was expressed as N-terminal DYKDDDDK
tagged protein (41 kDa) using baculovirus expression system.

IGF1R
Human IGF1R, cytoplasmic domain [959-1367(end) amino acids ofaccession number NP_000866.1] was expressed as N-terminal
GST-fusion protein (73 kDa) using baculovirus expression system.

IKKα(CHUK)
Full-length human IKKα [1-745(end) amino acids of accession
number NP_001269.3] was expressed as N-terminal GST-fusion
protein (111 kDa) using baculovirus expression system.

34

: MSA
: IRS1

ATP (μM) Km app / Bin : 63 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 40
IC50 at 1 mM ATP (nM) : 150

Assay platform
Substrate

Product code: 05-112: MSA: S6K2 peptide

ATP (μM) Km app / Bin : 22 / 25
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 6.9
IC50 at 1 mM ATP (nM) : 32

Assay platform
Substrate

Product code: 08-141: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 7 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 71
IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 07-410: MSA: DYRKtide-F: IMAP: IκBα peptide

ATP (μM) Km app / Bin : 41 / 40
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 310
IC50 at 1 mM ATP (nM) : n.a.

IKKβ(IKBKB)

Assay platform
Substrate

Product code: 05-084
Truncated human IKKβ[1-662 amino acids of accession number
NP_001547.1] was expressed as N-terminal His-tagged protein (77kDa) using baculovirus expression system.

IKKε(IKBKE)

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 410
IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 05-114
Full-length human IKKε [1-716(end) amino acids of accession
number NP_054721.1] was expressed as N-terminal GST-fusion
protein (108 kDa) using baculovirus expression system.

INSR
Human INSR, catalytic domain [1005-1310 amino acids ofaccession number NP_000199.1] was expressed as N-terminal
GST-fusion protein (62 kDa) using baculovirus expression system.

IRAK1
Truncated human IRAK1 [194-712(end) amino acids of accession
number NP_001560.2] was expressed as N-terminal GST-fusion
protein (83 kDa) using baculovirus expression system.

IRAK4Full-length human IRAK4 [1-460(end) amino acids of accession
number NP_057207.2] was expressed as N-terminal GST-fusion
protein (79 kDa) using baculovirus expression system.

35: IMAP: SRPKtide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 54
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 09-145: MSA: IRS1

ATP (μM) Km app / Bin : 58 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 12
IC50 at 1 mM ATP (nM) : 70

Assay platform
Substrate

Product code: 09-101: MSA: IκBα peptide

ATP (μM) Km app / Bin : 9.5 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.79IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-142: MSA: Modified IκBα-derived
peptide: MSA: IRAK1 peptide

ATP (μM) Km app / Bin : 920 / 1000
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 11
IC50 at 1 mM ATP (nM) : 11

IRR(INSRR)

Assay platform
Substrate

Product code: 08-143
Human IRR, cytoplasmic domain [953-1297(end) amino acids ofaccession number NP_055030.1] was expressed as N-terminal
GST-fusion protein (66 kDa) using baculovirus expression system.

ITK

ATP (μM) Km app / Bin : 64 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 15
IC50 at 1 mM ATP (nM) : 98

Assay platform
Substrate

Product code: 08-181
Full-length human ITK [2-620(end) amino acids of accession
number NP_005537.3] was expressed as N-terminal GST-fusion
protein (99 kDa) using baculovirus expression system.

JAK1
Human JAK1, catalytic domain [850-1154(end) amino acids ofaccession number NP_002218.2] was expressed as N-terminal
GST-fusion protein (62 kDa) using baculovirus expression system.

JAK2
Human JAK2, catalytic domain [826-1132(end) amino acids ofaccession number NP_004963.1] was expressed as N-terminal Histagged protein (39 kDa) using baculovirus expression system.

JAK3
Human JAK3, catalytic domain [795-1124(end) amino acids ofaccession number NP_000206.2] was expressed as N-terminal Histagged protein (41 kDa) using baculovirus expression system.

36

: MSA
: Srctide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.34
IC50 at 1 mM ATP (nM) : 6.0

Assay platform
Substrate

Product code: 08-046: MSA: JAK1 substrate peptide

ATP (μM) Km app / Bin : 68 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.71
IC50 at 1 mM ATP (nM) : 10

Assay platform
Substrate

Product code: 08-045: MSA: Srctide

ATP (μM) Km app / Bin : 6.1 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.2
IC50 at 1 mM ATP (nM) : 200

Assay platform
Substrate

Product code: 08-144: MSA: IRS1: MSA: Srctide

ATP (μM) Km app / Bin : 3.5 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.20IC50 at 1 mM ATP (nM) : 12

JNK1(MAPK8)

Assay platform
Substrate

Product code: 04-163
Human JNK1, catalytic domain [2-364 amino acids of accession
number NP_620634.1] was expressed as N-terminal GST-fusion
protein (69 kDa) using E. coli expression system. GST-JNK1 was
purified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K4 and MAP2K7. Activated GSTJNK1 was purified using glutathione sepharose chromatography.

JNK2(MAPK9)

ATP (μM) Km app / Bin : 29 / 100
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 99
IC50 at 1 mM ATP (nM) : 770

Assay platform
Substrate

Product code: 04-164
Human JNK2, catalytic domain [1-364 amino acids of accession
number NP_002743.3] was expressed as N-terminal GST-fusion
protein (69 kDa) using E. coli expression system. GST-JNK2 waspurified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K4 and MAP2K7. Activated GSTJNK2 was purified using Ni-NTA chromatography.

JNK3(MAPK10)
Full-length human JNK3 [1-426(end) amino acids of accession
number NP_620446.1] was expressed as N-terminal GST-fusion
protein (75 kDa) using E.coli expression system. GST-JNK3 waspurified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K4 and MAP2K7. Activated GSTJNK3 was purified using glutathione sepharose chromatography.

KDR
Human KDR, cytoplasmic domain [790-1356(end) amino acids ofaccession number NP_002244.1] was expressed as N-terminal
GST-fusion protein (90 kDa) using baculovirus expression system.

KIT
Human KIT, cytoplasmic domain [544-976(end) amino acids ofaccession number NP_000213.1] was expressed as N-terminal
GST-fusion protein (76 kDa) using baculovirus expression system.

37

: MSA
: CSKtide

ATP (μM) Km app / Bin : 74 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.1
IC50 at 1 mM ATP (nM) : 13

Assay platform
Substrate

Product code: 08-156: MSA: Modified Erktide

ATP (μM) Km app / Bin : 6 / 25
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 26
IC50 at 1 mM ATP (nM) : 730

Assay platform
Substrate

Product code: 08-191: MSA: Modified Erktide

ATP (μM) Km app / Bin : 21 / 50
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 110
IC50 at 1 mM ATP (nM) : 1600

Assay platform
Substrate

Product code: 04-150: MSA: Modified Erktide: MSA: Srctide

ATP (μM) Km app / Bin : 370 / 400
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.2
IC50 at 1 mM ATP (nM) : 2.0

KIT[D816E]

Assay platform
Substrate

Product code: 08-541
Human KIT, cytoplasmic domain [544-976(end) amino acids andD816E of accession number NP_000213.1] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

KIT[D816V]

ATP (μM) Km app / Bin : 40 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.7
IC50 at 1 mM ATP (nM) : 1.3

Assay platform
Substrate

Product code: 08-505
Human KIT, cytoplasmic domain [544-976(end) amino acids andD816V of accession number NP_000213.1] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

KIT[D816Y]
Human KIT, cytoplasmic domain [544-976(end) amino acids andD816Y of accession number NP_000213.1] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

KIT[T670I]
Human KIT, cytoplasmic domain [544-976(end) amino acids and
T670I of accession number NP_000213.1] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

KIT[V560G]
Human KIT, cytoplasmic domain [544-976(end) amino acids and
V560G of accession number NP_000213.1] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

38: MSA: Srctide

ATP (μM) Km app / Bin : 100 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.80IC50 at 1 mM ATP (nM) : 3.4

Assay platform
Substrate

Product code: 08-504: MSA: Srctide

ATP (μM) Km app / Bin : 22 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.27
IC50 at 1 mM ATP (nM) : 2.1

Assay platform
Substrate

Product code: 08-195: MSA: Srctide

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.18
IC50 at 1 mM ATP (nM) : 2.8

Assay platform
Substrate

Product code: 08-534: MSA: Srctide: MSA: Srctide

ATP (μM) Km app / Bin : 110 / 250
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.2
IC50 at 1 mM ATP (nM) : 1.6

KIT[V654A]

Assay platform
Substrate

Product code: 08-511
Human KIT, cytoplasmic domain [544-976(end) amino acids andV654A of accession number NP_000213.1] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

LATS1/MOBKL1A

ATP (μM) Km app / Bin : 220 / 250
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.5
IC50 at 1 mM ATP (nM) : 8.2

Assay platform
Substrate

Product code: 01-523
Human LATS1, catalytic domain [589-1130(end) amino acids ofaccession number NP_004681.1] was co-expressed as N-terminal
GST-fusion protein (90 kDa) with human His-tagged MOBKL1A [1216(end) amino acids of accession number NP_775739.1] andhuman BTN-MST2 [1-491(end) amino acids of accession number
NP_006272.2] using baculovirus expression system.

LATS2/MOBKL1AHuman LATS2, catalytic domain [553-1088(end) amino acids ofaccession number NP_055387.2] was co-expressed as N-terminal
GST-fusion protein (89 kDa) with human His-tagged MOBKL1A [1216(end) amino acids of accession number NP_775739.1] andhuman BTN-MST2 [1-491(end) amino acids of accession number
NP_006272.2] using baculovirus expression system.

LCK
Full-length human LCK [1-509(end) amino acids of accession
number NP_005347.2] was expressed as N-terminal GST-fusion
protein (85 kDa) using baculovirus expression system.

LOK(STK10)
Full-length human LOK [1-968(end) amino acids of accession
number BAA35073.1] was expressed as N-terminal GST-fusion
protein using baculovirus expression system. GST-LOK was
purified by using glutathione sepharose chromatography. GST-LOK
was cleaved by PreScission protease and GST-free LOK (114 kDa)
was collected as flow-through fraction from glutathione sepharose
chromatography.

39

: MSA
: Srctide

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.5
IC50 at 1 mM ATP (nM) : 14

Assay platform
Substrate

Product code: 07-315: MSA: SGKtide

ATP (μM) Km app / Bin : 38 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.7
IC50 at 1 mM ATP (nM) : 4.0

Assay platform
Substrate

Product code: 08-170: MSA: SGKtide

ATP (μM) Km app / Bin : 23 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.2
IC50 at 1 mM ATP (nM) : 11

Assay platform
Substrate

Product code: 01-524: MSA: Srctide: MSA: Moesin-derived peptide

ATP (μM) Km app / Bin : 100 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.49IC50 at 1 mM ATP (nM) : n.a.

LTK

Assay platform
Substrate

Product code: 08-106
Human LTK, catalytic domain [498-796 amino acids of accession
number NP_002335.2] was expressed as N-terminal GST-fusion
protein (60 kDa) using baculovirus expression system.

LYNa

ATP (μM) Km app / Bin : 49 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.0IC50 at 1 mM ATP (nM) : 7.1

Assay platform
Substrate

Product code: 08-171
Full-length human LYNa [1-512(end) amino acids of accession
number NP_002341.1] was expressed as N-terminal GST-fusion
protein (86 kDa) using baculovirus expression system.

LYNb
Full-length human LYNb [1-491(end) amino acids of accession
number NP_001104567.1] was expressed as N-terminal GSTfusion protein (83 kDa) using baculovirus expression system.

MAP4K2Full-length human MAP4K2 [1-820(end) amino acid of accession
number NP_004570.2] was expressed as N-terminal GST-fusion
protein (119 kDa) using baculovirus expression system.

MAPKAPK2
Full-length human MAPKAPK2 [1-400(end) amino acids ofaccession number NP_116584.2] was co-expressed as N-terminal
GST-fusion protein (73 kDa) with human His-tagged p38β [1364(end) amino acids of accession number NP_002742.3] andhuman His-tagged MAP2K6 [1-334(end) amino acids of accession
number NP_002749.2] using baculovirus expression system.

40

: MSA
: S6K2 peptide

ATP (μM) Km app / Bin : 93 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.3
IC50 at 1 mM ATP (nM) : 0.87

Assay platform
Substrate

Product code: 02-142: MSA: Srctide

ATP (μM) Km app / Bin : 18 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.0IC50 at 1 mM ATP (nM) : 21

Assay platform
Substrate

Product code: 07-111: MSA: Srctide

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.0IC50 at 1 mM ATP (nM) : 22

Assay platform
Substrate

Product code: 08-172: MSA: Srctide: MSA: GS peptide

ATP (μM) Km app / Bin : 3.6 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 80
IC50 at 1 mM ATP (nM) : 9300

MAPKAPK3

Assay platform
Substrate

Product code: 02-143
Full-length human MAPKAPK3 [1-382(end) amino acids ofaccession number NP_004626.1] was co-expressed as N-terminal
GST-fusion protein (70 kDa) with human His-tagged p38β [1364(end) amino acids of accession number NP_002742.3] andhuman His-tagged MAP2K6 [1-334(end) amino acids of accession
number NP_002749.2] using baculovirus expression system.

MAPKAPK5

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 410
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-144
Full-length human MAPKAPK5 [1-471(end) amino acids ofaccession number NP_003659.2] was co-expressed as N-terminal
GST-fusion protein (81 kDa) with human His-tagged p38β [1364(end) amino acids of accession number NP_002742.3] andhuman His-tagged MAP2K6 [1-334(end) amino acids of accession
number NP_002749] using baculovirus expression system.

MARK1
Full-length human MARK1 [1-795(end) amino acids of accession
number AAF72103.1] was expressed as N-terminal GST-fusion
protein ( 116 kDa) using baculovirus expression system.

MARK2
Full-length human MARK2 [1-745(end) amino acids of accession
number NP_059672.2] was expressed as N-terminal GST-fusion
protein (110 kDa) using baculovirus expression system.

MARK3
Full-length human MARK3 [1-729(end) amino acids of accession
number NP_002367.4] was expressed as N-terminal GST-fusion
protein (108 kDa) using baculovirus expression system.

41

: MSA
: CHKtide

ATP (μM) Km app / Bin : 8.8 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.12
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-122: MSA: CHKtide

ATP (μM) Km app / Bin : 8 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.17
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-121: MSA: GS peptide

ATP (μM) Km app / Bin : 12 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 320
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-120: MSA: GS peptide: MSA: CHKtide

ATP (μM) Km app / Bin : 5 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.20IC50 at 1 mM ATP (nM) : n.a.

MARK4

Assay platform
Substrate

Product code: 02-123
Full-length human MARK4 [1-688(end) amino acids of accession
number NP_113605.2] was expressed as N-terminal GST-fusion
protein (103 kDa) using baculovirus expression system.

MELK

ATP (μM) Km app / Bin : 12 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.12
IC50 at 1 mM ATP (nM) : 5.6

Assay platform
Substrate

Product code: 02-124
Truncated human MELK [1-493 amino acids of accession number
NP_055606.1] was expressed as N-terminal GST-fusion protein (83kDa) using E. coli expression system.

MER(MERTK)
Human MER, cytoplasmic domain [528-999(end) amino acids ofaccession number NP_006334.2] was expressed as N-terminal
GST-fusion protein (80 kDa) using baculovirus expression system.

MET
Human MET, cytoplasmic domain [956-1390(end) amino acids ofaccession number NP_000236.2] was expressed as N-terminal
GST-fusion protein (76 kDa) using baculovirus expression system.

MET[D1228H]
Human MET, cytoplasmic domain [956-1390(end) amino acids andD1228H of accession number NP_000236.2] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

42: MSA: Srctide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 67
IC50 at 1 mM ATP (nM) : 730

Assay platform
Substrate

Product code: 08-540: MSA: CSKtide

ATP (μM) Km app / Bin : 36 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.61
IC50 at 1 mM ATP (nM) : 5.3

Assay platform
Substrate

Product code: 08-151: MSA: GS peptide

ATP (μM) Km app / Bin : 38 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.81
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-108: MSA: CHKtide: MSA: Srctide

ATP (μM) Km app / Bin : 25 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 59
IC50 at 1 mM ATP (nM) : 1200

MET[M1250T]

Assay platform
Substrate

Product code: 08-545
Human MET, cytoplasmic domain [956-1390(end) amino acids andM1250T of accession number NP_000236.2] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

MET[Y1235D]

ATP (μM) Km app / Bin : 17 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 86
IC50 at 1 mM ATP (nM) : 1900

Assay platform
Substrate

Product code: 08-198
Human MET, cytoplasmic domain [956-1390(end) amino acids andY1235D of accession number NP_000236.2] was expressed as Nterminal GST-fusion protein (76 kDa) using baculovirus expression
system.

MINK(MINK1)
Human MINK, catalytic domain [1-314 amino acids of accession
number NP_056531.1] was expressed as N-terminal GST-fusion
protein (63 kDa) using baculovirus expression system.

MNK1(MKNK1)
Full-length human MNK1 [1-424(end) amino acids and T344D ofaccession number NP_001129025.1] was expressed as N-terminal
GST-fusion protein (74 kDa) using baculovirus expression system.

MNK2(MKNK2)
Full-length human MNK2 [1-465(end) amino acids and T379D ofaccession number NP_951009.1] was expressed as N-terminal
GST-fusion protein (79 kDa) using baculovirus expression system.

43

: MSA
: RS peptide

ATP (μM) Km app / Bin : 460 / 450
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 21
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-146: MSA: Modified Erktide

ATP (μM) Km app / Bin : 16 / 50
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 5.5
IC50 at 1 mM ATP (nM) : 4.7

Assay platform
Substrate

Product code: 02-145: MSA: Srctide

ATP (μM) Km app / Bin : 71 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 79
IC50 at 1 mM ATP (nM) : 390

Assay platform
Substrate

Product code: 07-139: MSA: Srctide: MSA: RS peptide

ATP (μM) Km app / Bin : 110 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 7.5
IC50 at 1 mM ATP (nM) : 44

MRCKα(CDC42BPA)

Assay platform
Substrate

Product code: 01-107
Truncated human MRCKα [1-574 amino acids of accession number
NP_003598.2] was expressed as N-terminal GST-fusion protein (93kDa) using baculovirus expression system.

MRCKβ(CDC42BPB)

ATP (μM) Km app / Bin : 0.45 / 1
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.2
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-108
Truncated human MRCKβ [1-473 amino acids of accession number
NP_006026.3] was expressed as N-terminal GST-fusion protein (82kDa) using baculovirus expression system.

MSK1(RPS6KA5)
Full-length human MSK1 [1-802(end) amino acids of accession
number NP_004746.2] was co-expressed as N-terminal GST-fusion
protein (117 kDa) with human His-tagged Erk2 [1-360 amino acidsof accession number NP_002736.3] using baculovirus expression
system.

MSK2(RPS6KA4)
Full-length human MSK2 [1-772(end) amino acids of accession
number NP_003933.1] was co-expressed as N-terminal GST-fusion
protein (114 kDa) with human His-tagged Erk2 [1-360 amino acidsof accession number NP_002736.3] using baculovirus expression
system.

MSSK1(STK23)
Full-length human MSSK1 [1-567(end) amino acids of accession
number NP_055185.2] was expressed as N-terminal GST-fusion
protein (89 kDa) using baculovirus expression system.

44

: MSA
: Crosstide

ATP (μM) Km app / Bin : 40 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.3
IC50 at 1 mM ATP (nM) : 20

Assay platform
Substrate

Product code: 04-159: MSA: Crosstide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.6
IC50 at 1 mM ATP (nM) : 30

Assay platform
Substrate

Product code: 01-148: MSA: DAPK1tide

ATP (μM) Km app / Bin : 0.67 / 1
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.6
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-147: MSA: DAPK1tide: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 56 / 50
Metal
: Mg
Reference compound : K252a
IC50 at ATP Bin (nM)
: 220
IC50 at 1 mM ATP (nM) : n.a.

MST1(STK4)

Assay platform
Substrate

Product code: 07-116
Full-length human MST1 [1-487(end) amino acids of accession
number NP_006273.1] was expressed as N-terminal GST-fusion
protein (83 kDa) using baculovirus expression system.

MST2(STK3)

ATP (μM) Km app / Bin : 50 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 0.55

Assay platform
Substrate

Product code: 07-117
Full-length human MST2 [1-491(end) amino acids of accession
number NP_006272.2] was expressed as N-terminal GST-fusion
protein (83 kDa) using baculovirus expression system.

MST3(STK24)
Full-length human MST3 [1-431(end) amino acids of accession
number NP_001027467.2] was expressed as N-terminal GSTfusion protein (75 kDa) using baculovirus expression system.

MST4
Full-length human MST4 [1-416(end) amino acids of accession
number NP_057626.2] was expressed as N-terminal GST-fusion
protein ( 74 kDa) using baculovirus expression system.

MUSK
Human MUSK, catalytic domain [527-869(end) amino acids ofaccession number NP_005583.1] was expressed as N-terminal
GST fusion protein (66 kDa) using baculovirus expression system.

45

: MSA
: Moesin-derived peptide

ATP (μM) Km app / Bin : 76 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 6.3
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-153: MSA: Moesin-derived peptide

ATP (μM) Km app / Bin : 66 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.9
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 07-119: MSA: IRS1

ATP (μM) Km app / Bin : 69 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 6.7
IC50 at 1 mM ATP (nM) : 3.1

Assay platform
Substrate

Product code: 07-118: MSA: IRS1: MSA: CSKtide

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.1
IC50 at 1 mM ATP (nM) : 2.6

NDR1(STK38)

Assay platform
Substrate

Product code: 01-125
Full-length human NDR1[1-465(end) amino acids of accession
number NP_009202.1] was co-expressed as N-terminal GST-fusion
protein (81kDa) with human His-tagged MOBKL1A [1-216(end)amino acids of accession number NP_775739.1] using baculovirus
expression system.

NDR2(STK38L)

ATP (μM) Km app / Bin : 12 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.8
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-126
Full-length human NDR2 [1-464(end) amino acids of accession
number NP_055815.1] was co-expressed as N-terminal GST-fusion
protein (81 kDa) with human His-tagged MOBKL1A [1-216(end)amino acids of accession number NP_775739.1] using baculovirus
expression system.

NEK1
Human NEK1, catalytic domain [1-505 amino acids of accession
number NP_036356.1] was expressed as N-terminal GST-fusion
protein (85 kDa) using baculovirus expression system.

NEK2
Full-length human NEK2 [1-445(end) amino acids of accession
number NP_002488.1] was expressed as N-terminal His-tagged
protein (55 kDa) using baculovirus expression system. His-tagged
NEK2 was purified by using Ni-NTA affinity chromatography.
Purified His-NEK2 was digested by recombinant His-TEV protease,and His-tag free NEK2 (ca. 52 kDa) was collected as flow-throughfraction from Ni-NTA affinity chromatography.

NEK4
Full-length human NEK4 [1-841(end) amino acids of accession
number NP_003148.2] was expressed as N-terminal GST-fusion
protein (122 kDa) using baculovirus expression system.

46

: MSA
: CDK7 peptide

ATP (μM) Km app / Bin : 65 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3700IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 05-128: MSA: CDK7 peptide

ATP (μM) Km app / Bin : 64 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 51
IC50 at 1 mM ATP (nM) : 650

Assay platform
Substrate

Product code: 05-226: MSA: SGKtide

ATP (μM) Km app / Bin : 7.6 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.1
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-123: MSA: SGKtide: MSA: GS peptide

ATP (μM) Km app / Bin : 51 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 120
IC50 at 1 mM ATP (nM) : n.a.

NEK6

Assay platform
Substrate

Product code: 05-130
Full-length human NEK6 [1-313(end) amino acids of accession
number NP_055212.2] was expressed as N-terminal GST-fusion
protein (63 kDa) using baculovirus expression system.

NEK7

ATP (μM) Km app / Bin : 69 / 75
Metal
: Mg
Reference compound : PKR Inhibitor
IC50 at ATP Bin (nM)
: 19000
IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 05-131
Full-length human NEK7 [1-302(end) amino acids of accession
number NP_598001.1] was expressed as N-terminal GST-fusion
protein (62 kDa) using baculovirus expression system.

NEK9Truncated human NEK9 [1-346, 733-979(end) amino acids ofaccession number NP_149107.4] was expressed as N-terminal
GST-fusion protein (93 kDa) using baculovirus expression system.

NIM1K(MGC42105)
Full-length human NIM1K [1-436(end) amino acids of accession
number NP_699192.1] was expressed as N-terminal GST-fusion
protein (76 kDa) using baculovirus expression system.

NuaK1
Full-length human NuaK1 [1-661(end) amino acids of accession
number NP_055655.1] was expressed as N-terminal GST-fusion
protein (102 kDa) using baculovirus expression system.

47

: MSA
: CHKtide

ATP (μM) Km app / Bin : 21 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 300
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-126: MSA: CDK7 peptide

ATP (μM) Km app / Bin : 190 / 200
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 150
IC50 at 1 mM ATP (nM) : 400

Assay platform
Substrate

Product code: 02-175: MSA: CDK7 peptide

ATP (μM) Km app / Bin : 40 / 50
Metal
: Mg
Reference compound : PKR Inhibitor
IC50 at ATP Bin (nM)
: 8500IC50 at 1 mM ATP (nM) : >10000

Assay platform
Substrate

Product code: 05-133: MSA: CDK7 peptide: MSA: CHKtide

ATP (μM) Km app / Bin : 59 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 3.4

NuaK2

Assay platform
Substrate

Product code: 02-127
Full-length human NuaK2 [1-628(end) amino acids of accession
number NP_112214.3] was expressed as N-terminal GST-fusion
protein (98kDa) using baculovirus expression system.

p38α(MAPK14)

ATP (μM) Km app / Bin : 26 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.2
IC50 at 1 mM ATP (nM) : 2.3

Assay platform
Substrate

Product code: 04-152
Truncated human p38α [9-352 amino acids of accession number
NP_620581.1] was expressed as N-terminal GST-fusion protein (66kDa) using E. coli expression system. GST-p38α was purified byusing glutathione sepharose chromatography and activated with
His-tagged MAP2K6. Activated GST-p38α was purified using
glutathione sepharose chromatography.

p38β(MAPK11)
Full-length human p38β[1-364(end) amino acids of accession
number NP_002742.3] was expressed as N-terminal GST-fusion
protein (69 kDa) using E. coli expression system.

p38γ(MAPK12)
Full-length human p38γ [1-367(end) amino acids of accession
number NP_002960.2] was expressed as N-terminal GST-fusion
protein (69 kDa) using E. coli expression system. GST-p38γ was
purified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K6. Activated GST-p38γ was
purified using glutathione sepharose chromatography.

p38δ(MAPK13)
Full-length human p38δ [1-365(end) amino acids of accession
number NP_002745.1] was expressed as N-terminal GST-fusion
protein (69 kDa) using E. coli expression system. GST-p38δ was
purified by using glutathione sepharose chromatography andactivated with His-tagged MAP2K6. Activated GST-p38δ was
purified using glutathione sepharose chromatography.

48

: MSA
: Modified Erktide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 88
IC50 at 1 mM ATP (nM) : 2800

Assay platform
Substrate

Product code: 04-154: MSA: Modified Erktide

ATP (μM) Km app / Bin : 63 / 75
Metal
: Mg
Reference compound : SB202190
IC50 at ATP Bin (nM)
: 16
IC50 at 1 mM ATP (nM) : 110

Assay platform
Substrate

Product code: 04-155: MSA: Modified Erktide

ATP (μM) Km app / Bin : 150 / 150
Metal
: Mg
Reference compound : SB202190
IC50 at ATP Bin (nM)
: 6.3
IC50 at 1 mM ATP (nM) : 22

Assay platform
Substrate

Product code: 04-153: MSA: CHKtide: MSA: Modified Erktide

ATP (μM) Km app / Bin : 5.8 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 220
IC50 at 1 mM ATP (nM) : >10000

p70S6K(RPS6KB1)

Assay platform
Substrate

Product code: 01-154
Human p70S6K, catalytic domain [1-421 amino acids and T412E ofaccession number NP_003152.1] was expressed as N-terminal
GST-fusion protein (75 kDa) using baculovirus expression system.

p70S6Kβ(RPS6KB2)

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.1
IC50 at 1 mM ATP (nM) : 9.8

Assay platform
Substrate

Product code: 01-155
Full-length human p70S6Kβ [1-482(end) amino acids of accession
number NP_003943.2] was expressed as N-terminal GST-fusion
protein (81 kDa) using baculovirus expression system.

PAK1
Full-length human PAK1 [1-545(end) amino acids of accession
number NP_002567.3] was expressed as N-terminal GST-fusion
protein (88 kDa) using baculovirus expression system.

PAK2
Full-length human PAK2 [1-524(end) amino acids of accession
number NP_002568.2] was expressed as N-terminal GST-fusion
protein (85 kDa) using baculovirus expression system.

PAK4
Full-length human PAK4 [1-591(end) amino acids of accession
number NP_005875.1] was expressed as N-terminal GST-fusion
protein (91 kDa) using baculovirus expression system.

49

: MSA
: DAPK1tide

ATP (μM) Km app / Bin : 81 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.5
IC50 at 1 mM ATP (nM) : 22

Assay platform
Substrate

Product code: 07-126: MSA: LIMKtide

ATP (μM) Km app / Bin : 300 / 300
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.0
IC50 at 1 mM ATP (nM) : 11

Assay platform
Substrate

Product code: 07-124: MSA: S6K2 peptide

ATP (μM) Km app / Bin : 3.3 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.7
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 07-123: MSA: S6K2 peptide: MSA: SGKtide

ATP (μM) Km app / Bin : 2.5 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 12
IC50 at 1 mM ATP (nM) : n.a.

PAK5(PAK7)

Assay platform
Substrate

Product code: 07-127
Human PAK5, catalytic domain [425-719(end) amino acids ofaccession number NP_065074.1] was expressed as N-terminal
GST-fusion protein (60 kDa) using baculovirus expression system.

PAK6

ATP (μM) Km app / Bin : 1.9 / 1
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.5
IC50 at 1 mM ATP (nM) : 290

Assay platform
Substrate

Product code: 07-128
Full-length human PAK6 [1-681(end) amino acids of accession
number NP_064553.1] was expressed as N-terminal GST-fusion
protein (102 kDa) using baculovirus expression system.

PASK
Human PASK, catalytic domain [949-1323(end) amino acids ofaccession number NP_055963.2] was expressed as N-terminal
GST-fusion protein (69 kDa) using baculovirus expression system.

PBK
Full-length human PBK [1-322(end) amino acids of accession
number NP_060962.2] was expressed as N-terminal GST-fusion
protein (63 kDa) using baculovirus expression system.

PDGFRα(PDGFRA)
Human PDGFRα, cytoplasmic domain [550-1089(end) amino acidsof accession number NP_006197.1] was expressed as N-terminal
GST-fusion protein(89 kDa) using baculovirus expression system.

50

: MSA
: Histone H3 peptide

ATP (μM) Km app / Bin : 33 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 69
IC50 at 1 mM ATP (nM) : 720

Assay platform
Substrate

Product code: 08-157: MSA: GS peptide

ATP (μM) Km app / Bin : 9.7 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 13
IC50 at 1 mM ATP (nM) : 190

Assay platform
Substrate

Product code: 05-168: MSA: SGKtide

ATP (μM) Km app / Bin : 3.7 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.2
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-128: MSA: DAPK1tide: MSA: CSKtide

ATP (μM) Km app / Bin : 28 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.30IC50 at 1 mM ATP (nM) : 1.4

PDGFRα(PDGFRA)[D842V]

Assay platform
Substrate

Product code: 08-506
Human PDGFRα, cytoplasmic domain [550-1089(end) amino acids
and D842V of accession number NP_006197.1] was expressed as
N-terminal GST-fusion protein (89 kDa) using baculovirus
expression system.

PDGFRα(PDGFRA)[T674I]

ATP (μM) Km app / Bin : 21 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.25
IC50 at 1 mM ATP (nM) : 1.9

Assay platform
Substrate

Product code: 08-503: MSA: CSKtide: MSA: CSKtide

Human PDGFRα, cytoplasmic domain [550-1089(end) amino acids
and T674I of accession number NP_006197.1] was expressed as N- ATP (μM) Km app / Bin : 11 / 10
terminal GST-fusion protein (89 kDa) using baculovirus expression
Metal
: Mg
system.

Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.12
IC50 at 1 mM ATP (nM) : 1.1

PDGFRα(PDGFRA)[V561D]

Assay platform
Substrate

Product code: 08-507
Human PDGFRα, cytoplasmic domain [550-1089(end) amino acids
and V561D of accession number NP_006197.1] was expressed as
N-terminal GST-fusion protein (89 kDa) using baculovirus
expression system.

PDGFRβ(PDGFRB)

ATP (μM) Km app / Bin : 35 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.32
IC50 at 1 mM ATP (nM) : 1.6

Assay platform
Substrate

Product code: 08-158
Human PDGFRβ, cytoplasmic domain [557-1106(end) amino acidsof accession number NP_002600.1] was expressed as N-terminal
GST-fusion protein (88 kDa) using baculovirus expression system.

PDHK2(PDK2)
Full-length human PDHK2 [1-407(end) amino acids of accession
number NP_002602.2] was expressed as N-terminal GST-fusion
protein (74 kDa) using baculovirus expression system.

51

: MSA
: CSKtide

ATP (μM) Km app / Bin : 23 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.27
IC50 at 1 mM ATP (nM) : 0.62

Assay platform
Substrate

Product code: 10-140: MSA: CSKtide: MSA: PDHKtide

ATP (μM) Km app / Bin : 28 / 25
Metal
: Mg+K
Reference compound : VER-246608
IC50 at ATP Bin (nM)
: 33
IC50 at 1 mM ATP (nM) : n.a.

PDHK4(PDK4)

Assay platform
Substrate

Product code: 10-125
Full-length human PDHK4 [1-411(end) amino acids of accession
number NP_002603.1] was expressed as N-terminal GST-fusion
protein (73 kDa) using E.coli expression system.

PDK1(PDPK1)

ATP (μM) Km app / Bin : 19 / 25
Metal
: Mg+K
Reference compound : VER-246608
IC50 at ATP Bin (nM)
: 120
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-132
Full-length human PDK1 [1-556(end) amino acids of accession
number NP_002604.1] was expressed as N-terminal GST-fusion
protein (91 kDa) using baculovirus expression system.

PEK(EIF2AK3)
Human PEK, cytoplasmic domain [536-1116(end) amino acids ofaccession number NP_004827.3] was expressed as N-terminal
GST-fusion protein (94 kDa) using E.coli expression system.

PGK(PRKG1)
Full-length human PGK [1-686(end) amino acids of accession
number NP_006249.1] was expressed as N-terminal GST-fusion
protein (105 kDa) using baculovirus expression system.

PHKG1
Full-length human PHKG1 [1-387(end) amino acids of accession
number NP_006204.1] was expressed as N-terminal GST-fusion
protein (72 kDa) using baculovirus expression system.

52

: MSA
: Kemptide

ATP (μM) Km app / Bin : 8.2 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.1
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-152: IMAP: SRPKtide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3600IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-142: MSA: T308tide

ATP (μM) Km app / Bin : 9.6 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 9.2
IC50 at 1 mM ATP (nM) : 12

Assay platform
Substrate

Product code: 05-155: MSA: PDHKtide: MSA: GS peptide

ATP (μM) Km app / Bin : 71 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.22
IC50 at 1 mM ATP (nM) : n.a.

PHKG2

Assay platform
Substrate

Product code: 02-153
Full-length human PHKG2 [1-406(end) amino acids of accession
number NP_000285.1] was expressed as N-terminal GST-fusion
protein (74 kDa) using baculovirus expression system.

PIK3CA/PIK3R1

ATP (μM) Km app / Bin : 8.1 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.74
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-401-20N
Full-length human PIK3CA[1-1068(end) amino acids of accession
number NP_006209.2] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (128 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIK3CA[E542K]/PIK3R1
Full-length human PIK3CA[1-1068(end) amino acids and E542K ofaccession number NP_006209.2] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (128 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIK3CA[E545K]/PIK3R1
Full-length human PIK3CA[1-1068(end) amino acids and E545K ofaccession number NP_006209.2] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (128 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIK3CA[H1047R]/PIK3R1
Full-length human PIK3CA[1-1068(end) amino acids and H1047R
of accession number NP_006209.2] was co-expressed as Nterminal DYKDDDDK tagged, biotinylated protein (128 kDa) with
PIK3R1[1-724(end) amino acids of accession number
NP_852664.1] using baculovirus expression system.

53: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 44 / 50
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 11
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-415-20N: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 42 / 50
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 12
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-414-20N: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 89 / 100
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 22
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-413-20N: MSA: GS peptide: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 78 / 75
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 10
IC50 at 1 mM ATP (nM) : n.a.

PIK3CA[P539R]/PIK3R1

Assay platform
Substrate

Product code: 11-412-20N
Full-length human PIK3CA[1-1068(end) amino acids and P539R ofaccession number NP_006209.2] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (128 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIK3CA[R88Q]/PIK3R1

ATP (μM) Km app / Bin : 37 / 50
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 8.7
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-411-20N
Full-length human PIK3CA[1-1068(end) amino acids and R88Q ofaccession number NP_006209.2] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (128 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIK3CB/PIK3R1
Full-length human PIK3CB[1-1070(end) amino acids of accession
number NP_006210.1] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (126 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIK3CD/PIK3R1
Full-length human PIK3CD[1-1044(end) amino acids of accession
number NP_005017.3] was co-expressed as N-terminalDYKDDDDK tagged, biotinylated protein (123 kDa) with PIK3R1[1724(end) amino acids of accession number NP_852664.1] using
baculovirus expression system.

PIKFYVE(PIP5K3)
Full-length human PIKFYVE [1-2098(end) amino acids and S696N,
L932S, Q995L, T998S, S1033A and Q1183K of accession number
NP_055855.2] was expressed as N-terminal GST-fusion protein(265 kDa) using baculovirus expression system.

54: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 37 / 50
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 24
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-118: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 88 / 100
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 22
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-403-20N: ADP-Glo: PI(4,5)P2

ATP (μM) Km app / Bin : 42 / 50
Metal
: Mg
Reference compound : PI-103
IC50 at ATP Bin (nM)
: 16
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-402-20N: ADP-Glo: PI(4,5)P2: ADP-Glo: PI(3)PATP (μM) Km app / Bin : 36 / 50
Metal
: Mg
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 3900IC50 at 1 mM ATP (nM) : n.a.

PIM1

Assay platform
Substrate

Product code: 02-054
Full-length human PIM1 [1-313(end) amino acids of accession
number NP_002639.1] was expressed as N-terminal His-tagged
protein (39 kDa) using baculovirus expression system.

PIM2

ATP (μM) Km app / Bin : 640 / 500
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 10
IC50 at 1 mM ATP (nM) : 20

Assay platform
Substrate

Product code: 02-155
Full-length human PIM2 [1-311(end) amino acids of accession
number NP_006866.2] was expressed as N-terminal GST-fusion
protein (61 kDa) using baculovirus expression system.

PIM3
Full-length human PIM3 [1-326(end) amino acids and V300A ofaccession number NP_001001852.2] was expressed as N-terminal
GST-fusion protein (63 kDa) using baculovirus expression system.

PIP4K2A
Full-length human PIP4K2A [1-406(end) amino acids of accession
number NP_005019] was expressed as N-terminal GST-fusion
protein (73 kDa) using baculovirus expression system.

PIP4K2B
Full-length human PIP4K2B [1-416(end) amino acids of accession
number NP_003550] was expressed as N-terminal GST-fusion
protein (74 kDa) using baculovirus expression system.

55: ADP-Glo: PI(5)PATP (μM) Km app / Bin : 20 / 25
Metal
: Mg
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 7600IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-116: MSA: S6K2 peptide

ATP (μM) Km app / Bin : 130 / 150
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.36
IC50 at 1 mM ATP (nM) : 0.71

Assay platform
Substrate

Product code: 11-115: MSA: S6K2 peptide

ATP (μM) Km app / Bin : 4 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 14
IC50 at 1 mM ATP (nM) : 480

Assay platform
Substrate

Product code: 02-156: MSA: S6K2 peptide: ADP-Glo: PI(5)PATP (μM) Km app / Bin : 18 / 25
Metal
: Mn
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 48000
IC50 at 1 mM ATP (nM) : n.a.

PIP5K1A

Assay platform
Substrate

Product code: 11-111
Full-length human PIP5K1A [1-549(end) amino acids of accession
number NP_003548.1] was expressed as N-terminal GST-fusion
protein (88 kDa) using baculovirus expression system.

PIP5K1B

ATP (μM) Km app / Bin : 28 / 25
Metal
: Mg
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 10000
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-112
Full-length human PIP5K1B [1-540(end) amino acids of accession
number NP_003549.1] was expressed as N-terminal GST-fusion
protein (88 kDa) using baculovirus expression system.

PIP5K1C
Full-length human PIP5K1C [1-668(end) amino acids of accession
number NP_036530] was expressed as N-terminal GST-fusion
protein (101 kDa) using baculovirus expression system.

PIP5KL1
Full-length human PIP5KL1 [1-394(end) amino acids of accession
number NP_001128691.1] was expressed as N-terminal GSTfusion protein (72 kDa) using baculovirus expression system.

PKACα(PRKACA)
Full-length human PKACα [1-351(end) amino acids of accession
number NP_002721.1] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

56: ADP-Glo: PI(4)PATP (μM) Km app / Bin : 1 / 1
Metal
: Mg
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 2200IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-127: ADP-Glo: PI(4)PATP (μM) Km app / Bin : 33 / 50
Metal
: Mg
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 1900IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-114: ADP-Glo: PI(4)PATP (μM) Km app / Bin : 95 / 100
Metal
: Mg
Reference compound : AG-183
IC50 at ATP Bin (nM)
: 4300IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-113: ADP-Glo: PI(4)P: MSA: Kemptide

ATP (μM) Km app / Bin : 2.6 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.80IC50 at 1 mM ATP (nM) : 86

PKACβ(PRKACB)

Assay platform
Substrate

Product code: 01-128
Full-length human PKACβ [1-351(end) amino acids of accession
number NP_002722.1] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

PKACγ(PRKACG)

ATP (μM) Km app / Bin : 4.7 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 37

Assay platform
Substrate

Product code: 01-129
Full-length human PKACγ [1-351(end) amino acids of accession
number NP_002723.2] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

PKCα(PRKCA)
Full-length human PKCα [1-672(end) amino acids of accession
number NP_002728.1] was expressed as N-terminal GST-fusion
protein (104 kDa) using baculovirus expression system.

PKCβ1(PRKCB1)
Full-length human PKCβ1 [1-671(end) amino acids of accession
number NP_997700.1] was expressed as N-terminal GST-fusion
protein (104 kDa) using baculovirus expression system.

PKCβ2(PRKCB2)
Full-length human PKCβ2 [1-673(end) amino acids of accession
number NP_002729.2] was expressed as N-terminal GST-fusion
protein (104 kDa) using baculovirus expression system.

57

: MSA
: PKC peptide

ATP (μM) Km app / Bin : 79 / 75
Metal
: Mg+Ca
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.71
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-165: MSA: PKC peptide

ATP (μM) Km app / Bin : 36 / 50
Metal
: Mg+Ca
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.33
IC50 at 1 mM ATP (nM) : 3.6

Assay platform
Substrate

Product code: 01-134: MSA: Kemptide

ATP (μM) Km app / Bin : 4.5 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 3.1
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-133: MSA: Kemptide: MSA: PKC peptide

ATP (μM) Km app / Bin : 41 / 50
Metal
: Mg+Ca
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.43
IC50 at 1 mM ATP (nM) : n.a.

PKCγ(PRKCG)

Assay platform
Substrate

Product code: 01-137
Full-length human PKCγ [1-697(end) amino acids of accession
number NP_002730.1] was expressed as N-terminal GST-fusion
protein (106 kDa) using baculovirus expression system.

PKCδ(PRKCD)

ATP (μM) Km app / Bin : 74 / 75
Metal
: Mg+Ca
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.1
IC50 at 1 mM ATP (nM) : 11

Assay platform
Substrate

Product code: 01-135
Full-length human PKCδ [1-676(end) amino acids of accession
number NP_006245.2] was expressed as N-terminal GST-fusion
protein (105 kDa) using baculovirus expression system.

PKCε(PRKCE)
Full-length human PKCε [1-737(end) amino acids of accession
number NP_005391.1] was expressed as N-terminal GST-fusion
protein (111 kDa) using baculovirus expression system.

PKCζ(PRKCZ)
Full-length human PKCζ [1-592(end) amino acids of accession
number NP_002735.3] was expressed as N-terminal GST-fusion
protein (94kDa) using baculovirus expression system.

PKCη(PRKCH)
Full-length human PKCη [1-683(end) amino acids of accession
number NP_006246.2] was expressed as N-terminal GST-fusion
protein (105 kDa) using baculovirus expression system.

58

: MSA
: PKC peptide

ATP (μM) Km app / Bin : 11 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 55
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-138: MSA: PKC peptide

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.37
IC50 at 1 mM ATP (nM) : 1.8

Assay platform
Substrate

Product code: 01-141: MSA: PKC peptide

ATP (μM) Km app / Bin : 26 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.22
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-136: MSA: PKC peptide: MSA: PKC peptide

ATP (μM) Km app / Bin : 36 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.92
IC50 at 1 mM ATP (nM) : n.a.

PKCθ(PRKCQ)

Assay platform
Substrate

Product code: 01-140
Full-length human PKCθ [1-706(end) amino acids and P330L ofaccession number NP_006248.1] was expressed as N-terminal
GST-fusion protein (109 kDa) using baculovirus expression system.

PKCι(PRKCI)ATP (μM) Km app / Bin : 18 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.72
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-139
Full-length human PKCι[1-587(end) amino acids of accession
number NP_002731.3] was expressed as N-terminal GST-fusion
protein (94 kDa) using baculovirus expression system.

PKD1(PRKD1)
Full-length human PKD1 [1-912(end) amino acids of accession
number NP_002733.1] was expressed as N-terminal GST-fusion
protein (129 kDa) using baculovirus expression system.

PKD2(PRKD2)
Full-length human PKD2 [1-878(end) amino acids of accession
number NP_057541.2] was expressed as N-terminal GST-fusion
protein (124 kDa) using baculovirus expression system.

PKD3(PRKD3)
Full-length human PKD3 [1-890(end) amino acids of accession
number NP_005804.1] was expressed as N-terminal GST-fusion
protein (127 kDa) using baculovirus expression system.

59

: MSA
: GS peptide

ATP (μM) Km app / Bin : 26 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.1
IC50 at 1 mM ATP (nM) : 16

Assay platform
Substrate

Product code: 02-159: MSA: GS peptide

ATP (μM) Km app / Bin : 25 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.1
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-158: MSA: PKC peptide

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 13
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-157: MSA: PKC peptide: MSA: GS peptide

ATP (μM) Km app / Bin : 34 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.80IC50 at 1 mM ATP (nM) : n.a.

PKN1

Assay platform
Substrate

Product code: 01-144
Full-length human PKN1 [1-942(end) amino acids of accession
number NP_002732.3] was expressed as N-terminal GST-fusion
protein (132 kDa) using baculovirus expression system.

PKR(EIF2AK2)

ATP (μM) Km app / Bin : 19 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.15
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-156
Human PKR , catalytic domain [252-551(end) amino acids ofaccession number NP_002750.1] was expressed as N-terminal
GST-fusion protein (62 kDa) using baculovirus expression system.

PLK1
Full-length human PLK1 [1-603(end) amino acids of accession
number NP_005021.2] was expressed as N-terminal GST-fusion
protein (95 kDa) using baculovirus expression system.

PLK2
Full-length human PLK2 [1-685(end) amino acids of accession
number NP_006613.2] was expressed as N-terminal GST-fusion
protein (105 kDa) using baculovirus expression system.

PLK3
Human PLK3, catalytic domain [58-340 amino acids of accession
number NP_004064.2] was expressed as N-terminal GST-fusion
protein (59 kDa) using baculovirus expression system.

60: IMAP: CHK2 peptide

ATP (μM) Km app / Bin : 30 / 30
Metal
: Mg
Reference compound : GW843682X
IC50 at ATP Bin (nM)
: 4.8
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-159: MSA: CDC25ctide

ATP (μM) Km app / Bin : 5.6 / 5
Metal
: Mg
Reference compound : GW843682X
IC50 at ATP Bin (nM)
: 3.6
IC50 at 1 mM ATP (nM) : 47

Assay platform
Substrate

Product code: 05-158: IMAP: SRPKtide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 87
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-157: IMAP: S6K peptide: MSA: CDC25ctide

ATP (μM) Km app / Bin : 6.8 / 5
Metal
: Mg
Reference compound : GW843682X
IC50 at ATP Bin (nM)
: 33
IC50 at 1 mM ATP (nM) : 450

PRKX

Assay platform
Substrate

Product code: 01-130
Full-length human PRKX [1-358(end) amino acids of accession
number NP_005035.1] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

PYK2(PTK2B)

ATP (μM) Km app / Bin : 20 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.59IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-138
Full-length human PYK2 [1-967(end) amino acids of accession
number NP_775267.1] was expressed as N-terminal GST-fusion
protein (138 kDa) using baculovirus expression system.

QIK(SNF1LK2)
Full-length human QIK(SNF1LK2) [1-926(end) amino acids ofaccession number NP_056006.1] was expressed as N-terminal
GST-fusion protein (132 kDa) using baculovirus expression system.

RET
Human RET, cytoplasmic domain [658-1114(end) amino acids ofaccession number NP_066124.1] was expressed as N-terminal
GST-fusion protein(79 kDa) using baculovirus expression system.

RET[G691S]
Human RET, cytoplasmic domain [658-1114(end) amino acids and
G691S of accession number NP_066124.1] was expressed as Nterminal GST-fusion protein (79 kDa) using baculovirus expression
system.

61: MSA: CSKtide

ATP (μM) Km app / Bin : 7.5 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.3
IC50 at 1 mM ATP (nM) : 20

Assay platform
Substrate

Product code: 08-522: MSA: AMARA peptide

ATP (μM) Km app / Bin : 42 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.4
IC50 at 1 mM ATP (nM) : 2.9

Assay platform
Substrate

Product code: 08-159: MSA: Blk/Lyntide

ATP (μM) Km app / Bin : 56 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.2
IC50 at 1 mM ATP (nM) : 4.9

Assay platform
Substrate

Product code: 02-129: MSA: Kemptide: MSA: CSKtide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.1
IC50 at 1 mM ATP (nM) : 24

RET[M918T]

Assay platform
Substrate

Product code: 08-508
Human RET, cytoplasmic domain [658-1114(end) amino acids and
M918T of accession number NP_066124.1] was expressed as Nterminal GST-fusion protein (79 kDa) using baculovirus expression
system.

RET[S891A]

ATP (μM) Km app / Bin : 4.2 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.4
IC50 at 1 mM ATP (nM) : 81

Assay platform
Substrate

Product code: 08-523
Human RET, cytoplasmic domain [658-1114(end) amino acids and
S891A of accession number NP_066124.1] was expressed as Nterminal GST-fusion protein (79 kDa) using baculovirus expression
system.

RET[Y791F]
Human RET, cytoplasmic domain [658-1114(end) amino acids and
Y791F of accession number NP_066124.1] was expressed as Nterminal GST-fusion protein (79 kDa) using baculovirus expression
system.

ROCK1
Human ROCK1, catalytic domain [1-477 amino acids of accession
number NP_005397.1] was expressed as N-terminal GST-fusion
protein (82 kDa) using baculovirus expression system.

ROCK2
Human ROCK2, catalytic domain [1-553 amino acids of accession
number NP_004841.2] was expressed as N-terminal GST-fusion
protein (91 kDa) using baculovirus expression system.

62

: MSA
: LIMKtide

ATP (μM) Km app / Bin : 3.1 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.6
IC50 at 1 mM ATP (nM) : 73

Assay platform
Substrate

Product code: 01-110: MSA: CSKtide

ATP (μM) Km app / Bin : 29 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.5
IC50 at 1 mM ATP (nM) : 26

Assay platform
Substrate

Product code: 01-109: MSA: CSKtide

ATP (μM) Km app / Bin : 11 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.44
IC50 at 1 mM ATP (nM) : 9.6

Assay platform
Substrate

Product code: 08-521: MSA: CSKtide: MSA: LIMKtide

ATP (μM) Km app / Bin : 7.4 / 5
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.92
IC50 at 1 mM ATP (nM) : 21

RON(MST1R)

Assay platform
Substrate

Product code: 08-152
Human RON, cytoplasmic domain [979-1400(end) amino acids ofaccession number NP_002438.1] was expressed as N-terminal
GST-fusion protein (75kDa) using baculovirus expression system.

ROS(ROS1)

ATP (μM) Km app / Bin : 27 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 37
IC50 at 1 mM ATP (nM) : 550

Assay platform
Substrate

Product code: 08-163
Human ROS, cytoplasmic domain [1883-2347(end) amino acids ofaccession number NP_002935.2] was expressed as N-terminal
GST-fusion protein (79 kDa) using baculovirus expression system.

RSK1(RPS6KA1)
Full-length human RSK1 [1-735(end) amino acids of accession
number NP_002944.2] was expressed as N-terminal GST-fusion
protein (110 kDa) using baculovirus expression system.

RSK2(RPS6KA3)
Full-length human RSK2 [1-740(end) amino acids of accession
number NP_004577.1] was expressed as N-terminal GST-fusion
protein (111 kDa) using baculovirus expression system.

RSK3(RPS6KA2)
Full-length human RSK3 [1-733(end) amino acids of accession
number NP_066958.2] was expressed as N-terminal GST-fusion
protein (111 kDa) using baculovirus expression system.

63

: MSA
: S6K peptide(N-FL)

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.10IC50 at 1 mM ATP (nM) : 2.1

Assay platform
Substrate

Product code: 01-151: MSA: S6K peptide(N-FL)

ATP (μM) Km app / Bin : 21 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.14
IC50 at 1 mM ATP (nM) : 2.5

Assay platform
Substrate

Product code: 01-150: MSA: IRS1

ATP (μM) Km app / Bin : 37 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.4
IC50 at 1 mM ATP (nM) : 1.0

Assay platform
Substrate

Product code: 01-149: MSA: Srctide: MSA: S6K peptide(N-FL)

ATP (μM) Km app / Bin : 9.9 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.11
IC50 at 1 mM ATP (nM) : 1.7

RSK4(RPS6KA6)

Assay platform
Substrate

Product code: 01-152
Full-length human RSK4 [1-745(end) amino acids of accession
number NP_055311.1] was expressed as N-terminal GST-fusion
protein (111 kDa) using baculovirus expression system.

SGK

ATP (μM) Km app / Bin : 20 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.051
IC50 at 1 mM ATP (nM) : 0.56

Assay platform
Substrate

Product code: 01-158
Truncated human SGK [61-431(end) amino acids and S422D ofaccession number NP_005618.2] was co-expressed as N-terminal
GST-fusion protein (68 kDa) with His-tagged PDK1 [1-556(end)amino acids of accession number NP_002604.1] using baculovirus
expression system.

SGK2
Full-length human SGK2 [1-367(end) amino acids and S356D ofaccession number NP_733794.1] was co-expressed as N-terminal
GST-fusion protein (68 kDa) with His-tagged PDK1 [1-556(end)amino acids of accession number NP_002604.1] using baculovirus
expression system.

SGK3(SGKL)
Truncated human SGK3 [119-496(end) amino acids and S486D ofaccession number NP_037389.4] was co-expressed as N-terminal
GST-fusion protein (68 kDa) with His-tagged PDK1 [1-556(end)amino acids of accession number NP_002604.1] using baculovirus
expression system.

SIK(SNF1LK)
Full-length human SIK [1-783(end) amino acids of accession
number NP_775490.2] was expressed as N-terminal GST-fusion
protein (112 kDa) using baculovirus expression system.

64

: MSA
: SGKtide

ATP (μM) Km app / Bin : 17 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 42
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-131: MSA: SGKtide

ATP (μM) Km app / Bin : 58 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 30
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 01-160: MSA: SGKtide

ATP (μM) Km app / Bin : 52 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 10
IC50 at 1 mM ATP (nM) : 99

Assay platform
Substrate

Product code: 01-159: MSA: S6K peptide(N-FL): MSA: AMARA peptide

ATP (μM) Km app / Bin : 47 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.8
IC50 at 1 mM ATP (nM) : 1.0

skMLCK(MYLK2)

Assay platform
Substrate

Product code: 02-150
Full-length human skMLCK [1-596(end) amino acids of accession
number NP_149109.1] was expressed as N-terminal GST-fusion
protein (93 kDa) using baculovirus expression system.

SLK

ATP (μM) Km app / Bin : 820 / 1000
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 51
IC50 at 1 mM ATP (nM) : 51

Assay platform
Substrate

Product code: 07-129
Full-length human SLK [1-1152(end) amino acids and S5N ofaccession number NP_055535.1] was expressed as N-terminal
GST-fusion protein (160 kDa) using baculovirus expression system.

SPHK1
Full-length human SPHK1 [1-384(end) amino acids of accession
number NP_001136074.1] was expressed as N-terminal GSTfusion protein (69 kDa) using baculovirus expression system.

SPHK2
Full-length human SPHK2 [1-618(end) amino acids of accession
number NP_001191089.1] was expressed as N-terminal GSTfusion protein (92 kDa) using baculovirus expression system.

SRC
Full-length human SRC [1-536(end) amino acids of accession
number NP_005408.1] was expressed as N-terminal GST-fusion
protein (87 kDa) using baculovirus expression system.

65: ADP-Glo: Sphingosine

ATP (μM) Km app / Bin : 200 / 200
Metal
: Mg
Reference compound : PF-543
IC50 at ATP Bin (nM)
: 1400IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-173: ADP-Glo: Sphingosine

ATP (μM) Km app / Bin : 5.9 / 5
Metal
: Mg
Reference compound : PF-543
IC50 at ATP Bin (nM)
: 17
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-106: MSA: Moesin-derived peptide

ATP (μM) Km app / Bin : 36 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.32
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 11-105: MSA: MLCtide: MSA: Srctide

ATP (μM) Km app / Bin : 31 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 5.3
IC50 at 1 mM ATP (nM) : 33

SRM(SRMS)

Assay platform
Substrate

Product code: 08-174
Human SRM, catalytic domain [215-488(end) amino acids ofaccession number NP_543013.1] was expressed as N-terminal
GST-fusion protein (58kDa) using baculovirus expression system.

SRPK1

ATP (μM) Km app / Bin : 38 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 290
IC50 at 1 mM ATP (nM) : 5000

Assay platform
Substrate

Product code: 04-160
Full-length human SRPK1 [1-655(end) amino acids and V504
deletion of accession number NP_003128.3] was expressed as Nterminal GST-fusion protein (101 kDa) using E. coli expression
system.

SRPK2Full-length human SRPK2 [1-688(end) amino acids of accession
number NP_872633.1] was expressed as N-terminal GST-fusion
protein (104 kDa) using baculovirus expression system.

SYK
Full-length human SYK [1-635(end) amino acids of accession
number NP_003168.2] was expressed as N-terminal GST-fusion
protein (99 kDa) using baculovirus expression system.

TAK1-TAB1(MAP3K7)
Fused gene of human TAK1 [1-303 amino acids of accession
number NP_663304.1] and human TAB1 [437-504 amino acids ofaccession number NP_006107.1] was expressed as N-terminal Histagged protein (45kDa) using baculovirus expression system.

66

: MSA
: Blk/Lyntide

ATP (μM) Km app / Bin : 59 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.29IC50 at 1 mM ATP (nM) : 0.63

Assay platform
Substrate

Product code: 09-019: MSA: DYRKtide-F

ATP (μM) Km app / Bin : 14 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 600
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-176: IMAP: SRPKtide

ATP (μM) Km app / Bin : 200 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 85
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 04-161: MSA: Blk/Lyntide: MSA: LRRKtide

ATP (μM) Km app / Bin : 37 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 12
IC50 at 1 mM ATP (nM) : 27

TAOK2

Assay platform
Substrate

Product code: 07-133
Human TAOK2, catalytic domain [1-319 amino acid of accession
number NP_004774.1] was expressed as N-terminal GST-fusion
protein (63 kDa) using baculovirus expression system.

TBK1

ATP (μM) Km app / Bin : 39 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 24
IC50 at 1 mM ATP (nM) : 100

Assay platform
Substrate

Product code: 05-115
Full-length human TBK1 [1-729(end) amino acids of accession
number NP_037386.1] was expressed as N-terminal GST-fusion
protein (111 kDa) using baculovirus expression system.

TEC
Human TEC, catalytic domain [359-631(end) amino acids ofaccession number NP_003206.2] was expressed as N-terminal
GST-fusion protein (59 kDa) using baculovirus expression system.

TIE2(TEK)
Human TIE2, cytoplasmic domain [771-1124(end) amino acids ofaccession number NP_000450.1] was expressed as N-terminal
GST-fusion protein (68 kDa) using baculovirus expression system.

TNIK
Human TNIK, catalytic domain [1-314 amino acids of accession
number NP_055843.1] was expressed as N-terminal GST-fusion
protein (62 kDa) using baculovirus expression system.

67

: MSA
: Blk/Lyntide

ATP (μM) Km app / Bin : 94 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 100
IC50 at 1 mM ATP (nM) : 190

Assay platform
Substrate

Product code: 07-138: MSA: Srctide

ATP (μM) Km app / Bin : 55 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 20
IC50 at 1 mM ATP (nM) : 220

Assay platform
Substrate

Product code: 08-185: MSA: CKtide

ATP (μM) Km app / Bin : 21 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.2
IC50 at 1 mM ATP (nM) : 6.2

Assay platform
Substrate

Product code: 08-182: MSA: TAOKtide: MSA: Moesin-derived peptide

ATP (μM) Km app / Bin : 16 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 11

TNK1

Assay platform
Substrate

Product code: 08-104
Human TNK1, catalytic domain [106-390 amino acids of accession
number Q13470-2] was expressed as N-terminal GST-fusion
protein (58 kDa) using baculovirus expression system.

TRKA(NTRK1)

ATP (μM) Km app / Bin : 71 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.55
IC50 at 1 mM ATP (nM) : 1.7

Assay platform
Substrate

Product code: 08-186
Human TRKA, cytoplasmic domain [436-790(end) amino acids ofaccession number NP_001012331.1] was expressed as N- terminal
GST-fusion protein (67 kDa) using baculovirus expression system.

TRKB(NTRK2)
Human TRKB, cytoplasmic domain [456-822(end) amino acids ofaccession number NP_001018074.1] was expressed as N- terminal
GST-fusion protein (69 kDa) using baculovirus expression system.

TRKC(NTRK3)
Human TRKC, cytoplasmic domain [456-825(end) amino acids ofaccession number NP_002521.2] was expressed as N-terminal
GST-fusion protein (69 kDa) using baculovirus expression system.

TSSK1
Full-length human TSSK1 [1-367(end) amino acids of accession
number NP_114417.1] was expressed as N-terminal GST-fusion
protein using baculovirus expression system. GST-TSSK1 was
purified by using glutathione sepharose chromatography. GSTTSSK1 was cleaved by PreScission protease and GST-free TSSK1(42 kDa) was collected as flow-through fraction from glutathionesepharose chromatography.

68

: MSA
: Srctide

ATP (μM) Km app / Bin : 47 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.32
IC50 at 1 mM ATP (nM) : 1.0

Assay platform
Substrate

Product code: 02-364: MSA: Srctide

ATP (μM) Km app / Bin : 80 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.29IC50 at 1 mM ATP (nM) : 0.55

Assay platform
Substrate

Product code: 08-197: MSA: CSKtide

ATP (μM) Km app / Bin : 65 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.34
IC50 at 1 mM ATP (nM) : 0.64

Assay platform
Substrate

Product code: 08-187: MSA: CSKtide: MSA: GS peptide

ATP (μM) Km app / Bin : 11 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.19IC50 at 1 mM ATP (nM) : 0.95

TSSK2

Assay platform
Substrate

Product code: 02-165
Full-length human TSSK2 [1-358(end) amino acids of accession
number NP_443732.3] was expressed as N-terminal GST-fusion
protein (68 kDa) using baculovirus expression system.

TSSK3

ATP (μM) Km app / Bin : 8.8 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 4.7
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 02-166
Full-length human TSSK3 [2-268(end) amino acids of accession
number NP_443073.1] was expressed as N-terminal GST-fusion
protein (57 kDa) using baculovirus expression system.

TXK
Human TXK, catalytic domain [260-527(end) amino acids ofaccession number NP_003319.2] was expressed as N-terminal
GST-fusion protein (58 kDa) using baculovirus expression system.

TYK2
Human TYK2, catalytic domain [871-1187(end) amino acids ofaccession number NP_003322.3] was expressed as N-terminal
GST-fusion protein (63 kDa) using baculovirus expression system.

TYRO3
Human TYRO3, cytoplasmic domain of [453-890(end) amino acidsof accession number NP_006284.2] was expressed as N-terminal
GST fusion protein (76 kDa) using baculovirus expression system.

69

: MSA
: Srctide

ATP (μM) Km app / Bin : 18 / 25
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.0
IC50 at 1 mM ATP (nM) : 7.0

Assay platform
Substrate

Product code: 08-109: MSA: Srctide

ATP (μM) Km app / Bin : 110 / 100
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 45
IC50 at 1 mM ATP (nM) : 220

Assay platform
Substrate

Product code: 08-147: MSA: GS peptide

ATP (μM) Km app / Bin : 45 / 50
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 12
IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-183: MSA: GS peptide: MSA: CSKtide

ATP (μM) Km app / Bin : 80 / 75
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.3
IC50 at 1 mM ATP (nM) : 2.9

WNK1

Assay platform
Substrate

Product code: 05-179
Human WNK1, catalytic domain [1-491 amino acids of accession
number NP_061852.1] was expressed as N-terminal GST-fusion
protein (81 kDa) using baculovirus expression system.

WNK2

ATP (μM) Km app / Bin : 140 / 150
Metal: Mg+Mn
Reference compound : K252a
IC50 at ATP Bin (nM)
: 4500IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-180
Human WNK2, catalytic domain [166-489 amino acids of accession
number NP_006639.3] was expressed as N-terminal GST-fusion
protein (65 kDa) using baculovirus expression system.

WNK3
Human WNK3, catalytic domain [1-434 amino acids of accession
number NP_065973.2] was expressed as N-terminal GST-fusion
protein (76 kDa) using baculovirus expression system.

YES(YES1)
Full-length human YES [1-543(end) amino acids of accession
number NP_005424.1] was expressed as N-terminal GST-fusion
protein (88 kDa) using baculovirus expression system.

YES(YES1)[T348I]
Full-length human YES [1-543(end) amino acids and T348I ofaccession number NP_005424.1] was expressed as N-terminal
GST-fusion protein (89 kDa) using baculovirus expression system.

70

: MSA
: Srctide

ATP (μM) Km app / Bin : 13 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 2.4
IC50 at 1 mM ATP (nM) : 23

Assay platform
Substrate

Product code: 08-533: MSA: SPAKtide

ATP (μM) Km app / Bin : 48 / 50
Metal
: Mg+Mn
Reference compound : K252a
IC50 at ATP Bin (nM)
: 1300IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 08-175: MSA: SPAKtide

ATP (μM) Km app / Bin : 48 / 50
Metal
: Mg+Mn
Reference compound : K252a
IC50 at ATP Bin (nM)
: 2300IC50 at 1 mM ATP (nM) : n.a.

Assay platform
Substrate

Product code: 05-181: MSA: SPAKtide: MSA: Srctide

ATP (μM) Km app / Bin : 8.5 / 10
Metal
: Mg
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 1.4
IC50 at 1 mM ATP (nM) : 45

ZAP70

Assay platform
Substrate

Product code: 08-177
Full-length human ZAP70 [1-619(end) amino acids of accession
number NP_001070] was expressed as N-terminal GST-fusion
protein (97 kDa) using baculovirus expression system.

71

: MSA
: Blk/Lyntide

ATP (μM) Km app / Bin : 3.3 / 5
Metal: Mg+Mn
Reference compound : Staurosporine
IC50 at ATP Bin (nM)
: 0.76
IC50 at 1 mM ATP (nM) : 34

BRAF

Assay platform
Substrate

Product code: 09-122
Human BRAF, catalytic domain [433-726 amino acid of accession
number NP_004324.2] was expressed as N-terminal GST-fusion
protein (60 kDa) using baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : ZM336372
IC50 at 1 mM ATP (nM) : >10000* MAP2K1/Erk2/Modified Erktide

BRAF[V600E]

Assay platform
Substrate

Product code: 09-144
Human BRAF, catalytic domain [433-726 amino acids and V600E
of accession number NP_004324.2] was expressed as N-terminal
GST-fusion protein (60 kDa) using baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : ZM336372
IC50 at 1 mM ATP (nM) : 662* MAP2K1/Erk2/Modified Erktide

COT(MAP3K8)

Assay platform
Substrate

Product code: 07-301
Human COT, catalytic domain [30-397 amino acids of accession
number NP_005195.2] was expressed as N-terminal GST-fusion
protein using baculovirus expression system. GST-COT was
purified by using glutathione sepharose chromatography. GST-COT
was cleaved by PreScission protease and GST-free COT (42 kDa)
was collected as flow-through fraction from glutathione sepharose
chromatography.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 120* MAP2K1/Erk2/Modified Erktide

DLK(MAP3K12)

Assay platform
Substrate

Product code: 09-111
Human DLK, catalytic domain [1-520 amino acid of accession
number NP_006292.3] was expressed as N-terminal GST-fusion
protein (86 kDa) using baculovirus expression system.

: MSA: MAP2K4/MAP2K7
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 460* (MAP2K4/MAP2K7)/JNK2/Modified Erktide

MAP2K1

Assay platform
Substrate

Product code: 07-141
Full-length human MAP2K1 [1-393(end) amino acids of accession
number NP_002746.1] was co-expressed as N-terminal GST-fusion
protein (71 kDa) with human His-tagged RAF1 [306-648(end) aminoacids and Y340D and Y341D of accession number NP_002871.1]
using baculovirus expression system.

ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 58
* Erk2/Modified Erktide

72

: MSA
: Erk2
Cascade Assay *MAP2K2

Assay platform
Substrate

Product code: 07-142
Full-length human MAP2K2 [1-400(end) amino acids of accession
number NP_109587.1] was co-expressed as N-terminal GST-fusion
protein (71 kDa) with human His-tagged RAF1 [306-648(end) aminoacids and Y340D and Y341D of accession number NP_002871.1]
using baculovirus expression system.

: MSA: Erk2
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 54
* Erk2/Modified Erktide

MAP2K3

Assay platform
Substrate

Product code: 07-143
Full-length human MAP2K3 [1-347(end) amino acids of accession
number NP_659731.1] was co-expressed as N-terminal GST-fusion
protein (67 kDa) with human His-tagged MLK3 [99-398 amino acidsof accession number NP_002410.1] using baculovirus expression
system.

: MSA: p38αCascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 790* p38α/Modified Erktide

MAP2K4

Assay platform
Substrate

Product code: 07-144
Full-length human MAP2K4 [1-399(end) amino acids of accession
number NP_003001.1] was co-expressed as N-terminal GST-fusion
protein (71 kDa) with human His-tagged MAP3K3 [1-626(end)amino acids of accession number NP_002392.2] using baculovirus
expression system.

: MSA: JNK2
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 4600
* JNK2/Modified Erktide

MAP2K5

Assay platform
Substrate

Product code: 07-145
Full-length human MAP2K5 [1-448(end) amino acids of accession
number NP_660143.1] was co-expressed as N-terminal GST-fusion
protein (77 kDa) with human His-tagged MAP3K3[1-626(end) aminoacids of accession number NP_002392.2] , CDC37 and HSP90
using baculovirus expression system.

: MSA: Erk5
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 62
* Erk5/EGFR-derived peptide

MAP2K6

Assay platform
Substrate

Product code: 07-146
Full-length human MAP2K6 [2-334(end) amino acids of accession
number NP_002749.2] was co-expressed as N-terminal GST-fusion
protein (64 kDa) with human His-tagged MLK3 [99-398 amino acidsof accession number NP_002410.1] using baculovirus expression
system.

ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 140* p38α/Modified Erktide

73

: MSA
: p38αCascade Assay *MAP2K7

Assay platform
Substrate

Product code: 07-148
Full-length human MAP2K7 [1-419(end) amino acids of accession
number NP_660186.1] was co-expressed as N-terminal GST-fusion
protein (75 kDa) with human His-tagged MAP3K3 [1-626(end)amino acids of accession number NP_002392.2] using baculovirus
expression system.

: MSA: JNK2
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 1100
* JNK2/Modified Erktide

MAP3K1

Assay platform
Substrate

Product code: 07-103
Human MAP3K1, catalytic domain [1193-1512(end) amino acids ofaccession number NP_005912.1] was expressed as N-terminal
GST-fusion protein (62 kDa) using baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 160* MAP2K1/Erk2/Modified Erktide

MAP3K2

Assay platform
Substrate

Product code: 07-104
Human MAP3K2, catalytic domain [336-619(end) amino acids ofaccession number NP_006600.3] was expressed as N-terminal
GST-fusion protein (59 kDa) using baculovirus expression system.

: MSA: MAP2K4/MAP2K7
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 45
* (MAP2K4/MAP2K7)/JNK2/Modified Erktide

MAP3K3

Assay platform
Substrate

Product code: 07-105
Full-length human MAP3K3 [1-626(end) amino acids of accession
number NP_002392.2] was expressed as N-terminal GST-fusion
protein (98 kDa) using baculovirus expression system.

: MSA: MAP2K6
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 72
* MAP2K6/p38α/Modified Erktide

MAP3K4

Assay platform
Substrate

Product code: 07-106
Human MAP3K4, catalytic domain [1312-1608(end) amino acids ofaccession number NP_005913.2] was expressed as N-terminal
GST-fusion protein (61 kDa) using baculovirus expression system.

: MSA: MAP2K6
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 100* MAP2K6/p38α/Modified Erktide

74

MAP3K5

Assay platform
Substrate

Product code: 07-107
Human MAP3K5, catalytic domain [654-971 amino acids ofaccession number NP_005914.1] was expressed as N-terminal
GST-tagged protein (62 kDa) using baculovirus expression system.

: MSA: MAP2K6
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 14
* MAP2K6/p38α/Modified Erktide

MLK1(MAP3K9)

Assay platform
Substrate

Product code: 09-115
Human MLK1, catalytic domain [110-422 amino acids of accession
number NP_149132.2] was expressed as N-terminal GST-fusion
protein (62kDa) using baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 11
* MAP2K1/Erk2/Modified Erktide

MLK2(MAP3K10)

Assay platform
Substrate

Product code: 09-116
Human MLK2, catalytic domain and leucine-zipper domain [75-462
amino acids of accession number NP_002437.2] was expressed as
N-terminal GST-fusion protein (71kDa) using baculovirus
expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 45
* MAP2K1/Erk2/Modified Erktide

MLK3(MAP3K11)

Assay platform
Substrate

Product code: 09-017
Human MLK3, catalytic domain [99-398 amino acids of accession
number NP_002410.1] was expressed as N-terminal His-tagged
protein (37kDa) using baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 4.8* MAP2K1/Erk2/Modified Erktide

MOS

Assay platform
Substrate

Product code: 05-118
Full-length, human MOS [1-346(end) amino acids of accession
number NP_005363.1] was expressed as N-terminal GST-fusion
protein (65 kDa) using baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : Staurosporine
IC50 at 1 mM ATP (nM) : 32
* MAP2K1/Erk2/Modified Erktide

75

RAF1

Assay platform
Substrate

Product code: 09-125
Human RAF1, catalytic domain [306-648(end) amino acids and
Y340D and Y341D of accession number NP_002871.1] wasexpressed as N-terminal GST-fusion protein (66 kDa) using
baculovirus expression system.

: MSA: MAP2K1
Cascade Assay *ATP (μM): 1000Metal: Mg
Reference compound : ZM336372
IC50 at 1 mM ATP (nM) : 2800
* MAP2K1/Erk2/Modified Erktide

76

Assay methods
Test compounds preparation
The test compound is dissolved in and diluted with dimethylsulfoxide (DMSO) to achieve 100-fold higher
concentration which is specified by the sponsor. Then the solution is further 25-fold diluted with assay buffer tomake the final test compound solution (4x compound solution). Reference compounds for the assay control areprepared similarly.

Assay reagents and procedures
Mobility Shift Assay (MSA)
1) 4x Substrate/ATP/Metal/Additive solution is prepared with kit buffer (20 mmol/L(M)HEPES, 0.01% Triton X-100, 5 mM DTT, pH7.5), and 2x kinase solution is preparedwith assay buffer (20 mM HEPES, 0.01% Triton X-100, 1 mM DTT, pH7.5).
2) 5 μL of 4x compound solution, 5 μL of 4x Substrate/ATP/Metal/Additive solution, and10 μL of 2x kinase solution are mixed and incubated in a well of polypropylene 384 well
microplate for 1 or 5 hour(s)* at room temperature. (*; depend on kinase)3) 70 μL of Termination Buffer (127 mM HEPES, 0.01% Triton X-100, 26.7 mM EDTA2Na, 1% DMSO, pH7.5) is added to the well.
4) The reaction mixture is applied to LabChip™ system (Revvity) or BioPhase™ 8800
system (AB Sciex), and the product and substrate peptide peaks are separated andquantitated.
5) The kinase reaction is evaluated by the product ratio calculated from peak heights (whenusing LabChip™ system) or area (when using BioPhase™ 8800 system) of product(P)and substrate(S) peptides (P/(P+S)).
Mobility Shift Assay (MSA) with pre-incubation
1) 4x Substrate/ATP/Metal/Additive solution is prepared with kit buffer (20 mM HEPES,
0.01% Triton X-100, 5 mM DTT, pH7.5), and 2x kinase solution is prepared with assay
buffer (20 mM HEPES, 0.01% Triton X-100, 1 mM DTT, pH7.5).
2) 5 μL of 4x compound solution and 10 μL of 2x kinase solution are mixed and incubatedin a well of polypropylene 384 well microplate for 30 minutes at room temperature.
3) 5 μL of 4x Substrate/ATP/Metal/Additive solution is added to the well, and incubated for
1 hour at room temperature.
4) 70 μL of Termination Buffer (127 mM HEPES, 0.01% Triton X-100, 26.7 mM EDTA2Na, 1% DMSO, pH7.5) is added to the well.
5) The reaction mixture is applied to LabChip™ system (Revvity) or BioPhase™ 8800
system (AB Sciex), and the product and substrate peptide peaks are separated andquantitated.
6) The kinase reaction is evaluated by the product ratio calculated from peak heights (whenusing LabChip™ system) or area (when using BioPhase™ 8800 system) of product(P)and substrate(S) peptides (P/(P+S)).

77

ADP-Glo™ Kinase Assay
1) 4x compound solution and 4x ATP solution are prepared with assay buffer (50 mM
MOPS, 1 mM DTT, pH7.2). 4x Substrate solution and 4x kinase/Metal solution areprepared with MOPS based buffer containing individual kinase specific additives.
2) 5 μL of 4x compound solution, 5 μL of 4x Substrate solution, 5 μL of 4x ATP solution,and 5 μL of 4x kinase/Metal solution are mixed and incubated in a well of polystyrene
384 well black microplate for 1 hour at room temperature.
3) 20 μL of ADP-Glo™ Reagent (Promega) is added to the well, and incubated for over 40
minutes.
4) 40 μL of Kinase Detection Reagent (Promega) is added to the well, and incubated forover 40 minutes.
5) The kinase reaction is evaluated by the endpoint luminescence of the well.
IMAP™ Assay
1) 4x Substrate/ATP/Metal solution and 2x kinase solution are prepared with assay buffer(20 mM HEPES, 0.01% Tween-20, 2 mM DTT, pH7.4).
2) 5 μL of 4x compound solution, 5 μL of 4x Substrate/ATP/Metal solution, and 10 μL of 2x
kinase solution are mixed and incubated in a well of polystyrene 384 well black
microplate for 1 hour at room temperature.
3) 60 μL of IMAP binding reagent (IMAP™ Screening Express kit; Molecular Devices) is
added to the well, and incubated for over 30 minutes.
4) The kinase reaction is evaluated by the fluorescence polarization at 485 nm for excitationand 530 nm for emission of the well.

Data analysis
The readout value of reaction control (complete reaction mixture) is set as a 0% inhibition, and the readout valueof background (Enzyme(-)) is set as a 100% inhibition, then the percent inhibition of each test solution is
calculated.
IC50 value is calculated from concentration vs. %Inhibition curves by fitting to a four parameter logistic curve.

78

Reaction conditions
ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

MSA

ABLtide

1000

16

25

1000

Mg

5

-

-

Staurosporine

1

ABL[E255K]

MSA

ABLtide

1000

17

25

1000

Mg

5

-

-

Staurosporine

1

ABL[T315I]

MSA

ABLtide

1000

4.0

5

1000

Mg

5

-

-

Staurosporine

1

ACK

MSA

WASP peptide

1000

97

100

1000

Mg

5

-

-

Staurosporine

5

AKT1

MSA

Crosstide

1000

31

50

1000

Mg

5

-

-

Staurosporine

1

AKT2

MSA

Crosstide

1000

110

100

-

Mg

5

-

-

Staurosporine

1

AKT3

MSA

Crosstide

1000

54

50

-

Mg

5

-

-

Staurosporine

1

ALK

MSA

Srctide

1000

57

50

1000

Mg

5

-

-

Staurosporine

1

ALK[C1156Y]

MSA

Srctide

1000

64

75

1000

Mg

5

-

-

Staurosporine

1

ALK[F1174L]

MSA

Srctide

1000

49

50

1000

Mg

5

-

-

Staurosporine

1

ALK[G1202R]

MSA

Srctide

1000

31

50

1000

Mg

5

-

-

Staurosporine

1

ALK[G1269A]

MSA

Srctide

1000

27

25

1000

Mg

5

-

-

Staurosporine

15

KinasePlatform

ABL

ALK[L1196M]

MSA

Srctide

1000

57

75

1000

Mg

-

-

Staurosporine

1

ALK[R1275Q]

MSA

Srctide

1000

84

100

1000

Mg

5

-

-

Staurosporine

1

ALK[T1151_L1152insT]

MSA

Srctide

1000

110

100

1000

Mg

5

-

-

Staurosporine1

EML4-ALK

MSA

Srctide

1000

43

50

1000

Mg

5

-

-

Staurosporine

5

NPM1-ALK

MSA

Srctide

1000

57

50

1000

Mg

5

-

-

Staurosporine1

AMPKα1/β1/γ1

MSA

SAMS peptide

1000

130

150

1000

Mg

5

-

-

Staurosporine1

AMPKα2/β1/γ1

MSA

SAMS peptide

1000

100

100

-

Mg

5

-

-

Staurosporine

1

ARG

MSA

ABLtide

1000

24

25

1000

Mg

5

-

-

Staurosporine

1

AurA

MSA

Kemptide

1000

27

25

1000

Mg

5

-

-

Staurosporine

1

AurA/TPX2

MSA

Kemptide

1000

1.7

2

-

Mg

5

TPX2

200 nM

Staurosporine

1

AurB/INCENP

MSA

Kemptide

1000

16

25

1000

Mg

5

-

-

Staurosporine

1

AurC

MSA

Kemptide

1000

24

25

1000

Mg

5

-

-

Staurosporine

1

AXL

MSA

CSKtide

1000

32

50

1000

Mg

5

-

-

Staurosporine

1

BLK

MSA

Srctide

1000

62

75

1000

Mg

5

-

-

Staurosporine

1

BMX

MSA

Srctide

1000

75

75

1000

Mg

5

-

-

Staurosporine

1

BRK

MSA

Blk/Lyntide

1000

250

250

1000

Mg

5

-

-

Staurosporine

5

BRSK1

MSA

CHKtide

1000

30

25

1000

Mg

5

-

-

Staurosporine

1

BRSK2

MSA

CHKtide

1000

31

50

-

Mg

5

-

-

Staurosporine

1

BTK

MSA

Srctide

1000

22

25

1000

Mg

5

-

-

Staurosporine

1

BTK[C481S]

MSA

Srctide

1000

27

25

1000

Mg

5

-

-

Staurosporine

179

ATP (μM)

Substrate

Metal

Additive

ReferencecompoundReactiontime (hour)

1 mM,
10 μg/ml
1 mM,
10 μg/ml
1 mM,
10 μg/ml
1 mM,
10 μg/ml
1 mM,
10 μg/ml
1 mM,
10 μg/ml
1 mM,
10 μg/ml-

Staurosporine

1

Staurosporine

5

Staurosporine

5

Staurosporine

1

Staurosporine

1

Staurosporine

1

Staurosporine

1

Staurosporine

1

Staurosporine

5

-

-

Staurosporine

1

5

-

-

Staurosporine

1

Mg

5

-

-

Staurosporine

1

1000

Mg

5

-

-

Staurosporine

1

200

1000

Mg

5

-

-

Staurosporine

5

10

1000

Mg

5

-

-

Staurosporine

1

330

300

1000

Mg

5

-

-

Staurosporine

5

1000

32

50

1000

Mg

5

-

-

Staurosporine

5

CDK9 substrate

1000

9.4

10

1000

Mg

5

-

-

Staurosporine

5MSA

Kemptide

1000

24

25

-

Mg

5

cGMP

5 μM

Staurosporine

1

MSA

CHKtide

1000

50

50

1000

Mg

5

-

-

Staurosporine

1

CHK2

MSA

CHKtide

1000

51

50

1000

Mg

5

-

-

Staurosporine

1

CK1α

MSA

CKtide

1000

4.1

5

1000

Mg

5

-

-

5-Iodotubercidin

5

CK1γ1

MSA

CKtide

1000

6.3

5

-

Mg

5

-

-

5-Iodotubercidin

1

CK1γ2

MSA

CKtide

1000

10

10

-

Mg

5

-

-

5-Iodotubercidin

1

CK1γ3

MSA

CKtide

1000

3.2

5

-

Mg

5

-

-

5-Iodotubercidin

1

CK1δ

MSA

CKtide

1000

7.7

10

1000

Mg

5

-

-

5-Iodotubercidin

1

CK1ε

MSA

CKtide

1000

16

25

1000

Mg

5

-

-

5-Iodotubercidin

5CK2α1/βMSA

CK2tide

1000

2.9

5

-

Mg

5

-

-

TBB

1

CK2α2/βMSA

CK2tide

1000

2.1

5

-

Mg

5

-

-

TBB

1

KinasePlatform

BUB1/BUB3

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

MSA

H2A peptide

1000

2.9

5

-

Mg

5

CaMK1αMSA

GS peptide

1000

750

1000

1000

Mg

5

CaMK1δ

MSA

Synapsin peptide

1000

11

10

-

Mg

5

CaMK2αMSA

GS peptide

1000

33

50

1000

Mg

5

CaMK2βMSA

GS peptide

1000

19

25

1000

Mg

5

CaMK2γMSA

GS peptide

1000

23

25

1000

Mg

5

CaMK2δ

MSA

GS peptide

1000

6.3

5

1000

Mg

5

CaMK4

MSA

GS peptide

1000

20

25

1000

Mg

5

CDC7/ASKMSA

MCM2 peptide

1000

2.8

5

1000

Mg

10

CaCl2,
Calmodulin
CaCl2,
Calmodulin
CaCl2,
Calmodulin
CaCl2,
Calmodulin
CaCl2,
Calmodulin
CaCl2,
Calmodulin
CaCl2,
Calmodulin-

CDK1(CDC2)/CycB1

MSA

Modified Histone H1

1000

34

50

1000

Mg

5

CDK2/CycA2

MSA

Modified Histone H1

1000

27

25

1000

Mg

CDK2/CycE1

MSA

Modified Histone H1

1000

130

150

1000

CDK3/CycE1

MSA

Modified Histone H1

1000

1000

1000

CDK4/CycD3MSA

DYRKtide-F

1000

200

CDK5/p25

MSA

Modified Histone H1

1000

10

CDK6/CycD3MSA

DYRKtide-F

1000

CDK7/CycH/MAT1

MSA

CTD3 peptide

CDK9/CycT1

MSA

CGK2
CHK1

80

ATP (μM)

Substrate

Metal

Additive

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

10

-

Mg

5

-

-

Staurosporine

1

150

1000

Mg

5

-

-

Staurosporine

1

-

Mg

5

-

-

Staurosporine

1

Mg

5

-

-

Staurosporine

5Mg, Mn5, 1--

Staurosporine

5

Mg

5

-

-

Staurosporine

1

-

Mg

5

-

-

Staurosporine

5

100

1000

Mg

5

-

-

Staurosporine

5

38

50

1000

Mg

5

-

-

Staurosporine

5

130

100

-

Mg

5

-

-

Non-disclosable

1

61

50

-

Mg

5

-

-

Non-disclosable

1

55

50

-

Mg

5

-

-

Non-disclosable

1

120

100

-

Mg

5

-

-

Non-disclosable

1

120

100

-

Mg

5

-

-

Non-disclosable

1

25

25

-

Mg

5

-

-

Non-disclosable

1

24

25

-

Mg

5

-

-

Non-disclosable

1

37

50

-

Mg

5

-

-

Non-disclosable

1

34

50

-

Mg

5

-

-

Non-disclosable

1

17

25

-

Mg

1

-

-

Non-disclosable

1

16

25

1000

Mg

5

-

-

Staurosporine

1

59

50

1000

Mg

5

-

-

Staurosporine

1

1000

7.7

10

1000

Mg

5

-

-

Staurosporine

1

DYRKtide-F

1000

6.8

5

1000

Mg

5

1

EEF2Ktide

1000

12

10

-

Mg

5

A-484954

5

EGFR

MSA

Srctide

1000

2.7

5

1000

Mg, Mn5, 1

1 mM,
10 μg/ml-

Staurosporine

MSA

CaCl2,
Calmodulin-

Staurosporine

1

EGFR[C797S/L858R]

MSA

Srctide

1000

4.1

5

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[d746-750]

MSA

Srctide

1000

19

25

1000

Mg, Mn5, 1--

Staurosporine

1

KinasePlatform

CLK1
CLK2

Name

(nM)

Km

Km BinMSA

DYRKtide-F

1000

11

MSA

DYRKtide-F

1000

140

CLK3

MSA

DYRKtide-F

1000

75

75

CRIK

MSA

Histone H3 peptide

1000

7.8

10

-

CSK

MSA

Srctide

1000

4.8

5

1000

DAPK1

MSA

DAPK1tide

1000

1.1

1

1000

DCAMKL2MSA

GS peptide

1000

120

150

DDR1

MSA

IRS1

1000

94

DDR2

MSA

DGKα

ADP-GloDGKβADP-GloDGKγADP-GloDGKδ

ADP-GloDGKεADP-GloDGKζ

ADP-GloDGKη

ADP-GloDGKθ

ADP-GloDGKι

ADP-GloDGKκ

ADP-GloDYRK1AMSA

IRS1Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,
POPS
Diacylglycerol,POPS
DYRKtide-F

1000
850000,6750000
850000,6750000
850000,6750000
850000,6750000
775000,1600000
850000,6750000
850000,6750000
850000,6750000
850000,6750000
67500,
8000001000

DYRK1BMSA

DYRKtide-F

1000

DYRK2

MSA

DYRKtide-F

DYRK3

MSA

EEF2K

81

ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

MSA

Srctide

1000

8.2

10

1000

Mg, Mn5, 1--

Staurosporine

1

MSA

Srctide

1000

5.4

5

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[d746-750/T790M/C797S]

MSA

Srctide

1000

1.8

2

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[D770_N771insNPG]

MSA

Srctide

1000

2.3

5

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[L858R]

MSA

Srctide

1000

9.8

10

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[L861Q]

MSA

Srctide

1000

7.5

10

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[T790M]

MSA

Srctide

1000

0.90

1

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[T790M/C797S/L858R]

MSA

Srctide

1000

0.85

-

1000

Mg, Mn5, 1--

Staurosporine

1

EGFR[T790M/L858R]

MSA

Srctide

1000

1.9

2

1000

Mg, Mn5, 1--

Staurosporine

1

EPHA1

MSA

Blk/Lyntide

1000

22

25

1000

Mg

5

-

-

Staurosporine

1

EPHA2

MSA

Blk/Lyntide

1000

67

75

1000

Mg

5

-

-

Staurosporine

1

EPHA3

MSA

Blk/Lyntide

1000

170

150

1000

Mg

5

-

-

Staurosporine

1

EPHA4

MSA

Blk/Lyntide

1000

52

50

1000

Mg

5

-

-

Staurosporine

1

EPHA5

MSA

Blk/Lyntide

1000

56

50

1000

Mg

5

-

-

Staurosporine

15

KinasePlatform

EGFR[d746-750/C797S]
EGFR[d746-750/T790M]

EPHA6

MSA

Blk/Lyntide

1000

27

25

1000

Mg

-

-

Staurosporine

1

EPHA7

MSA

Blk/Lyntide

1000

58

50

1000

Mg

5

-

-

Staurosporine

1

EPHA8

MSA

Blk/Lyntide

1000

69

75

1000

Mg

5

-

-

Staurosporine

1

EPHB1

MSA

Blk/Lyntide

1000

29

25

1000

Mg

5

-

-

Staurosporine

1

EPHB2

MSA

Blk/Lyntide

1000

86

100

1000

Mg

5

-

-

Staurosporine

1

EPHB3

MSA

Blk/Lyntide

1000

49

50

1000

Mg

5

-

-

Staurosporine

1

EPHB4

MSA

Blk/Lyntide

1000

56

50

1000

Mg

5

-

-

Staurosporine

1

Erk1

MSA

Modified Erktide

1000

34

50

1000

Mg

5

-

-

K252a

1

Erk2

MSA

Modified Erktide

1000

33

50

1000

Mg

5

-

-

K252a

1

Erk5

MSA

EGFR-derived peptide

1000

450

1000

1000

Mg

5

-

-

Staurosporine

5

FAK

MSA

Blk/Lyntide

1000

25

25

1000

Mg

5

-

-

Staurosporine

5

5

FER

MSA

Srctide

1000

26

25

1000

Mg

-

-

Staurosporine

1

FES

MSA

Srctide

1000

43

50

1000

Mg

5

-

-

Staurosporine

1

FGFR1

MSA

CSKtide

1000

89

100

1000

Mg

5

-

-

Staurosporine

1

FGFR1[V561M]

MSA

CSKtide

1000

33

50

1000

Mg

5

-

-

Staurosporine

1

FGFR2

MSA

CSKtide

1000

66

75

1000

Mg

5

-

-

Staurosporine

1

FGFR2[V564I]

MSA

CSKtide

1000

21

25

1000

Mg

5

-

-

Staurosporine

1

FGFR3

MSA

CSKtide

1000

43

50

1000

Mg

5

-

-

Staurosporine

1

FGFR3[K650E]

MSA

CSKtide

1000

41

50

1000

Mg

5

-

-

Staurosporine

1

FGFR3[K650M]

MSA

CSKtide

1000

17

25

1000

Mg

5

-

-

Staurosporine

182

ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

MSA

CSKtide

1000

29

25

1000

Mg

5

-

-

Staurosporine

1

MSA

CSKtide

1000

37

50

1000

Mg

5

-

-

Staurosporine

1

FGFR4

MSA

CSKtide

1000

230

250

1000

Mg

5

-

-

Staurosporine

1

FGFR4[N535K]

MSA

CSKtide

1000

30

25

1000

Mg

5

-

-

Staurosporine

1

FGFR4[V550E]

MSA

CSKtide

1000

210

200

1000

Mg

5

-

-

Staurosporine

1

FGFR4[V550L]

MSA

CSKtide

1000

160

150

1000

Mg

5

-

-

Staurosporine

1

FGR

MSA

Srctide

1000

34

50

1000

Mg

5

-

-

Staurosporine

1

FLT1

MSA

CSKtide

1000

140

150

1000

Mg

5

-

-

Staurosporine

1

FLT3

MSA

Srctide

1000

94

100

1000

Mg

5

-

-

Staurosporine

1

FLT4

MSA

CSKtide

1000

72

75

1000

Mg

5

-

-

Staurosporine

1

FMS

MSA

Srctide

1000

26

25

1000

Mg

5

-

-

Staurosporine

1

FRK

MSA

Srctide

1000

62

75

1000

Mg

5

-

-

Staurosporine

1

FYN[isoform a]

MSA

Srctide

1000

36

50

1000

Mg

5

-

-

Staurosporine

1

FYN[isoform b]

MSA

Srctide

1000

20

25

1000

Mg

5

-

-

Staurosporine

1

GSK3α

MSA

CREBtide-p

1000

12

10

1000

Mg

5

-

-

Staurosporine

1

GSK3β

MSA

CREBtide-p

1000

9.1

10

1000

Mg

5

-

-

Staurosporine

1

HaspinMSA

Histone H3 peptide

1000

140

150

-

Mg

5

-

-

Staurosporine

1

HCK

MSA

Srctide

1000

11

10

1000

Mg

5

-

-

Staurosporine

1

HER2

MSA

Srctide

1000

3.5

5

1000

Mn

5

-

-

Staurosporine

1

HER4

MSA

Srctide

1000

27

25

1000

Mg

5

-

-

Staurosporine

1

HGK

MSA

Moesin-derived peptide

1000

9.4

10

1000

Mg

5

-

-

Staurosporine

1

HIPK1

MSA

DYRKtide-F

1000

4.4

5

-

Mg

5

-

-

Staurosporine

1

HIPK2

MSA

DYRKtide-F

1000

5.9

5

-

Mg

5

-

-

Staurosporine

1

HIPK3

MSA

DYRKtide-F

1000

7.3

5

1000

Mg

5

-

-

Staurosporine

1

HIPK4

MSA

DYRKtide-F

1000

7.0

5

1000

Mg

5

-

-

Staurosporine

1

HPK1

MSA

S6K2 peptide

1000

22

25

1000

Mg

1.25

-

-

K252a

1

IGF1R

MSA

IRS1

1000

63

75

1000

Mg

5

-

-

Staurosporine

1

IKKα

IMAP

100

41

40

-

Mg

10

-

-

Staurosporine

1

IKKβ

MSA

1000

16

25

1000

Mg

5

-

-

Staurosporine

1

IKKε

MSA

IκBα peptide
Modified IκBα-derived
peptideIκBα peptide

1000

9.5

10

-

Mg

5

-

-

Staurosporine

5

INSR

MSA

IRS1

1000

58

50

1000

Mg

5

-

-

Staurosporine

1

IRAK1

IMAP

SRPKtide

100

27

25

-

Mg

2.5

-

-

Staurosporine

1

IRAK4

MSA

IRAK1 peptide

1000

920

1000

1000

Mg

5

-

-

Staurosporine

5

KinasePlatform

FGFR3[V555L]
FGFR3[V555M]

83

ATP (μM)

Substrate

Metal

AdditiveKm

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

1000

64

75

1000

Mg

5

-

-

Staurosporine

1

1000

6.1

10

1000

Mg

5

-

-

Staurosporine

1

JAK1 substrate peptide

1000

68

75

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

5

MSA

Srctide

1000

13

10

1000

Mg

5

-

-

Staurosporine

1

MSA

Srctide

1000

3.5

5

1000

Mg

5

-

-

Staurosporine

1

JNK1

MSA

Modified Erktide

1000

29

100

1000

Mg

5

-

-

K252a

1

JNK2

MSA

Modified Erktide

1000

21

50

1000

Mg

5

-

-

K252a

1

JNK3

MSA

Modified Erktide

1000

6.0

25

1000

Mg

5

-

-

K252a

1

KDR

MSA

CSKtide

1000

74

75

1000

Mg

5

-

-

Staurosporine

1

KIT

MSA

Srctide

1000

370

400

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

KIT[D816E]

MSA

Srctide

1000

40

50

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

KIT[D816V]

MSA

Srctide

1000

14

10

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

KIT[D816Y]

MSA

Srctide

1000

22

25

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

KIT[T670I]

MSA

Srctide

1000

100

100

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

KIT[V560G]

MSA

Srctide

1000

110

250

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

KIT[V654A]

MSA

Srctide

1000

220

250

1000

Mg

5

Sodium orthovanadate

25 μM

Staurosporine

1

LATS1/MOBKL1A

MSA

SGKtide

1000

23

25

1000

Mg

5

-

-

Staurosporine

5

LATS2/MOBKL1A

MSA

SGKtide

1000

38

50

1000

Mg

5

-

-

Staurosporine

5

LCK

MSA

Srctide

1000

14

10

1000

Mg

5

-

-

Staurosporine

1

LOK

MSA

Moesin-derived peptide

1000

100

100

-

Mg

5

-

-

Staurosporine

5

LTK

MSA

Srctide

1000

49

50

1000

Mg

5

-

-

Staurosporine

1

LYNa

MSA

Srctide

1000

14

10

1000

Mg

5

-

-

Staurosporine

1

LYNb

MSA

Srctide

1000

18

25

1000

Mg

5

-

-

Staurosporine

1

MAP4K2MSA

S6K2 peptide

1000

93

100

1000

Mg

5

-

-

Staurosporine

1

MAPKAPK2MSA

GS peptide

1000

3.6

5

1000

Mg

5

-

-

Staurosporine

15

KinasePlatform

IRR
ITK

Name

(nM)

MSA

IRS1

MSA

Srctide

JAK1

MSA

JAK2
JAK3

MAPKAPK3MSA

GS peptide

1000

13

10

-

Mg

-

-

K252a

1

MAPKAPK5MSA

GS peptide

1000

12

10

-

Mg

5

-

-

Staurosporine

1

MARK1

MSA

CHKtide

1000

8.0

10

-

Mg

5

-

-

Staurosporine

1

MARK2

MSA

CHKtide

1000

8.8

10

-

Mg

5

-

-

Staurosporine

1

MARK3

MSA

CHKtide

1000

5.0

5

-

Mg

5

-

-

Staurosporine

1

MARK4

MSA

CHKtide

1000

12

10

1000

Mg

5

-

-

Staurosporine

1

MELK

MSA

GS peptide

1000

38

50

-

Mg

5

-

-

Staurosporine

5

MER

MSA

CSKtide

1000

36

50

1000

Mg

5

-

-

Staurosporine

184

ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

MSA

Srctide

1000

27

25

1000

Mg

5

-

-

Staurosporine

1

MSA

Srctide

1000

25

25

1000

Mg

5

-

-

Staurosporine

1

MET[M1250T]

MSA

Srctide

1000

17

25

1000

Mg

5

-

-

Staurosporine

1

MET[Y1235D]

MSA

Srctide

1000

71

75

1000

Mg

5

-

-

Staurosporine

1

MINK

MSA

Modified Erktide

1000

16

50

1000

Mg

5

-

-

K252a

5

MNK1

MSA

RS peptide

1000

460

450

-

Mg

5

-

-

Staurosporine

1

MNK2

MSA

RS peptide

1000

110

100

1000

Mg

5

-

-

Staurosporine

1

MRCKα

MSA

DAPK1tide

1000

0.45

1

-

Mg

5

-

-

Staurosporine

5

MRCKβ

MSA

DAPK1tide

1000

0.67

1

-

Mg

5

-

-

Staurosporine

1

MSK1

MSA

Crosstide

1000

13

10

1000

Mg

5

-

-

Staurosporine

1

MSK2

MSA

Crosstide

1000

40

50

1000

Mg

5

-

-

Staurosporine

5

MSSK1

MSA

DYRKtide-F

1000

56

50

-

Mg

5

-

-

K252a

5

MST1

MSA

IRS1

1000

50

50

1000

Mg

5

Cantharidin

20 μM

Staurosporine

5

MST2

MSA

IRS1

1000

69

75

1000

Mg

5

Cantharidin

10 μM

Staurosporine

5

MST3

MSA

Moesin-derived peptide

1000

66

75

-

Mg

5

-

-

Staurosporine

5

MST4

MSA

Moesin-derived peptide

1000

76

75

-

Mg

5

-

-

Staurosporine

5

MUSK

MSA

CSKtide

1000

14

10

1000

Mg, Mn5, 1--

Staurosporine

5

NDR1

MSA

SGKtide

1000

12

10

-

Mg

5

-

-

Staurosporine

5

NDR2

MSA

SGKtide

1000

7.6

10

-

Mg

5

-

-

Staurosporine

5

NEK1

MSA

CDK7 peptide

1000

64

75

1000

Mg

5

-

-

Staurosporine

5

NEK2

MSA

CDK7 peptide

1000

65

75

1000

Mg

5

-

-

Staurosporine

1

NEK4

MSA

GS peptide

1000

51

50

-

Mg

5

-

-

Staurosporine

1

NEK6

MSA

CDK7 peptide

1000

69

75

1000

Mg

5

-

-

PKR Inhibitor

5

NEK7

MSA

CDK7 peptide

1000

40

50

1000

Mg

5

-

-

PKR Inhibitor

5

NEK9

MSA

CDK7 peptide

1000

190

200

1000

Mg

5

-

-

Staurosporine

5

NIM1K

MSA

CHKtide

1000

21

25

-

Mg

5

-

-

Staurosporine

1

NuaK1

MSA

CHKtide

1000

59

50

1000

Mg

5

-

-

Staurosporine

1

NuaK2

MSA

CHKtide

1000

26

25

1000

Mg

5

-

-

Staurosporine

1

p38α

MSA

Modified Erktide

1000

150

150

1000

Mg

5

-

-

SB202190

1

p38β

MSA

Modified Erktide

1000

63

75

1000

Mg

5

-

-

SB202190

1

p38γ

MSA

Modified Erktide

1000

13

10

1000

Mg

5

-

-

Staurosporine

1

p38δ

MSA

Modified Erktide

1000

5.8

5

1000

Mg

5

-

-

Staurosporine

1

p70S6KMSA

S6K2 peptide

1000

14

10

1000

Mg

5

-

-

Staurosporine

1

p70S6KβMSA

S6K2 peptide

1000

3.3

5

-

Mg

5

-

-

Staurosporine

1

KinasePlatform

MET
MET[D1228H]

85

ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)MSA

LIMKtide

1000

300

300

1000

Mg

5

-

-

Staurosporine

1

MSA

DAPK1tide

1000

81

100

1000

Mg

5

-

-

Staurosporine

1

PAK4

MSA

SGKtide

1000

2.5

5

-

Mg

5

-

-

Staurosporine

5

PAK5

MSA

DAPK1tide

1000

1.9

1

1000

Mg

5

-

-

Staurosporine

1

PAK6

MSA

SGKtide

1000

3.7

5

-

Mg

5

-

-

Staurosporine

5

PASK

MSA

GS peptide

1000

9.7

10

1000

Mg

5

-

-

Staurosporine

5

PBK

MSA

Histone H3 peptide

1000

33

50

1000

Mg

5

-

-

Staurosporine

5

PDGFRαMSA

CSKtide

1000

28

25

1000

Mg

5

-

-

Staurosporine1

PDGFRα[D842V]

MSA

CSKtide

1000

21

25

1000

Mg

5

-

-

Staurosporine1

PDGFRα[T674I]

MSA

CSKtide

1000

11

10

1000

Mg

5

-

-

Staurosporine

5

PDGFRα[V561D]

MSA

CSKtide

1000

35

50

1000

Mg

5

-

-

Staurosporine1

PDGFRβMSA

CSKtide

1000

23

25

1000

Mg

5

-

-

Staurosporine

1

PDHK2

MSA

PDHKtide

1000

28

25

-

Mg, K

5, 3

-

-

VER-246608

5

PDHK4

MSA

PDHKtide

1000

19

25

-

Mg, K

5, 25

5

MSA

T308tide

1000

9.6

10

1000

Mg

5

Staurosporine

5

PEK

IMAP

SRPKtide

100

13

10

-

Mg

5

2 μM,
20 μM
-

VER-246608

PDK1

PIFtide,Cantharidin-

Staurosporine

1

PGK

MSA

Kemptide

1000

8.2

10

-

Mg

5

cGMP

5 μM

Staurosporine

5

PHKG1

MSA

GS peptide

1000

71

75

-

Mg

5

-

-

Staurosporine

5

PHKG2

MSA

GS peptide
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(4,5)P2,
POPS
PI(3)P,
POPS

1000
10000,
5000
10000,
5000
10000,
5000
10000,
5000
10000,
5000
10000,
5000
10000,
5000
10000,
5000
10000,
20000

8.1

10

-

Mg

5

-

-

Staurosporine

1

89

100

-

Mg

5

-

-

PI-103

1

42

50

-

Mg

5

-

-

PI-103

1

44

50

-

Mg

5

-

-

PI-103

1

78

75

-

Mg

5

-

-

PI-103

1

37

50

-

Mg

5

-

-

PI-103

1

42

50

-

Mg

5

-

-

PI-103

1

88

100

-

Mg

5

-

-

PI-103

1

37

50

-

Mg

5

-

-

PI-103

1

36

50

-

Mg

5

-

-

AG-183

1

KinasePlatform

PAK1
PAK2

PIK3CA/PIK3R1

ADP-Glo

PIK3CA[E542K]/PIK3R1

ADP-Glo

PIK3CA[E545K]/PIK3R1

ADP-Glo

PIK3CA[H1047R]/PIK3R1

ADP-Glo

PIK3CA[P539R]/PIK3R1

ADP-Glo

PIK3CA[R88Q]/PIK3R1

ADP-Glo

PIK3CB/PIK3R1

ADP-Glo

PIK3CD/PIK3R1

ADP-Glo

PIKFYVE

ADP-Glo86ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)MSA

S6K2 peptide

1000

640

500

1000

Mg

5

-

-

Staurosporine

1

MSA

S6K2 peptide

1000

4.0

5

1000

Mg

5

-

-

Staurosporine

5

MSA

1000
10000,
20000
10000,
20000
10000,
20000
10000,
20000
10000,
20000
10000,
20000
1000

130

150

1000

Mg

5

-

-

Staurosporine

1

20

25

-

Mg

5

-

-

AG-183

1

18

25

-

Mn

0.25

-

-

AG-183

1

28

25

-

Mg

5

-

-

AG-183

1

95

100

-

Mg

5

-

-

AG-183

1

33

50

-

Mg

5

-

-

AG-183

1

1.0

1

-

Mg

5

-

-

AG-183

1

KinasePlatform

PIM1
PIM2
PIM3
PIP4K2A

ADP-Glo

PIP4K2B

ADP-Glo

PIP5K1A

ADP-Glo

PIP5K1B

ADP-Glo

PIP5K1C

ADP-Glo

PIP5KL1

ADP-Glo

PKACα

MSA

S6K2 peptide
PI(5)P,
POPS
PI(5)P,
POPS
PI(4)P,
POPS
PI(4)P,
POPS
PI(4)P,
POPS
PI(4)P,
POPS
Kemptide

2.6

5

1000

Mg

5

-

-

Staurosporine

1

PKACβ

MSA

Kemptide

1000

4.7

5

1000

Mg

5

-

-

Staurosporine

1

PKACγ

MSA

Kemptide

1000

4.5

5

-

Mg

5

5

MSA

PKC peptide

1000

36

50

1000

Mg, Ca5, 0.05

Staurosporine

1

PKCβ1

MSA

PKC peptide

1000

79

75

-

Mg, Ca5, 0.05

Staurosporine

1

PKCβ2

MSA

PKC peptide

1000

41

50

-

Mg, Ca5, 0.05

Staurosporine

1

PKCγ

MSA

PKC peptide

1000

74

75

1000

Mg, Ca5, 0.05

Staurosporine

1

PKCδ

MSA

PKC peptide

1000

26

25

-

Mg

5

Staurosporine

1

PKCε

MSA

PKC peptide

1000

16

25

1000

Mg

5

Staurosporine

1

PKCζ

MSA

PKC peptide

1000

11

10

-

Mg

5

Staurosporine

1

PKCη

MSA

PKC peptide

1000

36

50

-

Mg

5

Staurosporine

1

PKCθ

MSA

PKC peptide

1000

18

25

-

Mg

5

Staurosporine

1

PKCι

MSA

PKC peptide

1000

27

25

-

Mg

5

50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL
50 μg/mL,
5 μg/mL-

Staurosporine

PKCαPhosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol
Phosphatidylserine,
Diacyl Glycerol-

Staurosporine

1

PKD1

MSA

GS peptide

1000

25

25

-

Mg

5

-

-

Staurosporine

1

PKD2

MSA

GS peptide

1000

26

25

1000

Mg

5

-

-

Staurosporine

1

PKD3

MSA

GS peptide

1000

34

50

-

Mg

5

-

-

Staurosporine

187

ATP (μM)

Substrate

Metal

Additive

Name

(nM)

Km

Km Bin

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

IMAP

S6K peptide

100

19

25

-

Mg

1

-

-

Staurosporine

1

IMAP

SRPKtide

100

13

10

-

Mg

5

-

-

Staurosporine

1

PLK1

MSA

CDC25ctide

1000

5.6

5

1000

Mg

5

-

-

GW843682X

5

PLK2

IMAP

CHK2 peptide

50

30

30

-

Mg

10

-

-

GW843682X

1

PLK3

MSA

CDC25ctide

1000

6.8

5

1000

Mg

5

-

-

GW843682X

1

PRKX

MSA

Kemptide

1000

20

25

-

Mg

5

-

-

Staurosporine

5

PYK2

MSA

Blk/Lyntide

1000

56

50

1000

Mg

5

-

-

Staurosporine

1

QIK

MSA

AMARA peptide

1000

42

50

1000

Mg

5

-

-

Staurosporine

1

RET

MSA

CSKtide

1000

7.5

10

1000

Mg

5

-

-

Staurosporine

1

RET[G691S]

MSA

CSKtide

1000

13

10

1000

Mg

5

-

-

Staurosporine

1

RET[M918T]

MSA

CSKtide

1000

4.2

5

1000

Mg

5

-

-

Staurosporine

1

RET[S891A]

MSA

CSKtide

1000

11

10

1000

Mg

5

-

-

Staurosporine

1

RET[Y791F]

MSA

CSKtide

1000

29

25

1000

Mg

5

-

-

Staurosporine

1

ROCK1

MSA

LIMKtide

1000

3.1

5

1000

Mg

5

-

-

Staurosporine

1

ROCK2

MSA

LIMKtide

1000

7.4

5

1000

Mg

5

-

-

Staurosporine

1

RON

MSA

Srctide

1000

27

25

1000

Mg

5

-

-

Staurosporine

1

ROS

MSA

IRS1

1000

37

50

1000

Mg

5

-

-

Staurosporine

1

RSK1

MSA

S6K peptide(N-FL)

1000

21

25

1000

Mg

5

-

-

Staurosporine

1

RSK2

MSA

S6K peptide(N-FL)

1000

14

10

1000

Mg

5

-

-

Staurosporine

1

RSK3

MSA

S6K peptide(N-FL)

1000

9.9

10

1000

Mg

5

-

-

Staurosporine

1

RSK4

MSA

S6K peptide(N-FL)

1000

20

25

1000

Mg

5

-

-

Staurosporine

1

SGK

MSA

SGKtide

1000

52

50

1000

Mg

5

-

-

Staurosporine

1

SGK2

MSA

SGKtide

1000

58

50

-

Mg

5

-

-

Staurosporine

1

SGK3

MSA

SGKtide

1000

17

25

-

Mg

5

-

-

Staurosporine

1

SIK

MSA

AMARA peptide

1000

47

50

1000

Mg

5

5

MSA

MLCtide

1000

820

1000

1000

Mg

5

Staurosporine

1

SLK

MSA

50

-

Mg

5

Staurosporine

5

ADP-Glo

5.9

5

-

Mg

5

-

-

PF-543

1

SPHK2

ADP-Glo

200

200

-

Mg

5

-

-

PF-543

1

SRC

MSA

1000
10000,
20000
10000,
20000
1000

36

SPHK1

Moesin-derived peptide
Sphingosine,
POPS
Sphingosine,
POPS
Srctide

1 mM,
10 μg/ml-

Staurosporine

skMLCK

CaCl2,
Calmodulin
-

31

50

1000

Mg

5

-

-

Staurosporine

1

SRM

MSA

Blk/Lyntide

1000

38

50

1000

Mg

5

-

-

Staurosporine

1

SRPK1

IMAP

SRPKtide

100

200

100

-

Mg

10

-

-

Staurosporine

1

KinasePlatform

PKN1
PKR

88

ATP (μM)

Substrate

Metal

Additive

1mM

Name

(mM)

Name

Concentration

ReferencecompoundReactiontime (hour)

10

-

Mg

5

-

-

Staurosporine

5

50

1000

Mg

5

-

-

Staurosporine

1

37

50

1000

Mg

1.25

-

-

Staurosporine

1

1000

39

50

1000

Mg

5

Cantharidin

10 μM

Staurosporine

5

1000

21

25

1000

Mg

5

-

-

Staurosporine

1

Srctide

1000

55

50

1000

Mg

5

-

-

Staurosporine

1

MSA

Blk/Lyntide

1000

94

100

1000

Mg

5

-

-

Staurosporine

1

TNIK

MSA

Moesin-derived peptide

1000

16

25

1000

Mg

5

-

-

Staurosporine

1

TNK1

MSA

CSKtide

1000

71

75

1000

Mg

5

-

-

Staurosporine

5

TRKA

MSA

CSKtide

1000

65

75

1000

Mg

5

-

-

Staurosporine

1

TRKB

MSA

Srctide

1000

80

75

1000

Mg

5

-

-

Staurosporine

1

TRKC

MSA

Srctide

1000

47

50

1000

Mg

5

-

-

Staurosporine

1

TSSK1

MSA

GS peptide

1000

11

10

1000

Mg

5

-

-

Staurosporine

1

TSSK2

MSA

GS peptide

1000

8.8

10

-

Mg

5

-

-

Staurosporine

5

TSSK3

MSA

GS peptide

1000

45

50

-

Mg

5

-

-

Staurosporine

5

TXK

MSA

Srctide

1000

110

100

1000

Mg

5

-

-

Staurosporine

5

TYK2

MSA

Srctide

1000

18

25

1000

Mg

5

-

-

Staurosporine

5

TYRO3

MSA

CSKtide

1000

80

75

1000

Mg

5

-

-

Staurosporine

1

WNK1

MSA

SPAKtide

1000

140

150

-

Mg, Mn

5, 3

-

-

K252a

5

WNK2

MSA

SPAKtide

1000

48

50

-

Mg, Mn

5, 3

-

-

K252a

5

WNK3

MSA

SPAKtide

1000

48

50

-

Mg, Mn

5, 3

-

-

K252a

5

YES

MSA

Srctide

1000

13

10

1000

Mg

5

-

-

Staurosporine

1

YES[T348I]

MSA

Srctide

1000

8.5

10

1000

Mg

5

-

-

Staurosporine

1

ZAP70

MSA

Blk/Lyntide

1000

3.3

5

1000

Mg, Mn5, 1--

Staurosporine

1

KinasePlatform

SRPK2
SYK

Name

(nM)

Km

Km BinMSA

DYRKtide-F

1000

14

MSA

Blk/Lyntide

1000

59

TAK1-TAB1MSA

LRRKtide

1000

TAOK2

MSA

TAOKtide

TBK1

MSA

CKtide

TEC

MSA

TIE2

89

Reaction conditions of Cascade assay
Substrate

Metal

ReferencecompoundReactiontime (hour)

ZM336372

1

5

ZM336372

1

5

Staurosporine

1

Mg

5

Staurosporine

5

1000

Mg

5

Staurosporine

1

1000

1000

Mg

5

Staurosporine

1

1000

1000

Mg

5

Staurosporine

1

Modified Erktide

1000

1000

Mg

5

Staurosporine

5

EGFR-derived peptide

1000

1000

Mg

5

Staurosporine

5

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

Modified Erktide

1000

1000

Mg

5

Staurosporine5

2.5

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

JNK2

50

Modified Erktide

1000

1000

Mg

5

Staurosporine

5

p38α

10

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

p38α

10

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

p38α

10

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

MAP2K1

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

5

Staurosporine

1

MAP2K1

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

5

ZM336372

1

MAP2K

MAPK

ATP
(μM)

KinasePlatform

Peptide

Name

(nM)

Name

(nM)

Name

(nM)

Name

(mM)

BRAF

MSA

MAP2K1

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

5

BRAF[V600E]

MSA

MAP2K1

1

Erk2

2.5

Modified Erktide

1000

1000

Mg

COT

MSA

2.5

Modified Erktide

1000

1000

Mg

MSA

JNK2

50

Modified Erktide

1000

1000

MAP2K1

MSA

1
0.5,
0.5
-

Erk2

DLK

MAP2K1
MAP2K4,
MAP2K7
-

Erk2

2.5

Modified Erktide

1000

MAP2K2

MSA

-

-

Erk2

2.5

Modified Erktide

MAP2K3

MSA

-

-

p38α

10

Modified Erktide

MAP2K4

MSA

-

-

JNK2

50

MAP2K5

MSA

-

-

Erk5

50

MAP2K6

MSA

-

-

p38α

10

MAP2K7

MSA

-

-

JNK2

50

MAP3K1MSA
MSA

MAP3K3

MSA

1
0.5,
0.5
1

Erk2

MAP3K2

MAP2K1
MAP2K4,
MAP2K7
MAP2K6

MAP3K4MSA

MAP2K6

1

MAP3K5MSA

MAP2K6

1

MLK1

MSA

MAP2K1

1

MLK2

MSA

MAP2K1MLK3MSA

MAP2K1

MOS

MSA

RAF1

MSA

90

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