serine/threonine kinase 3 (MST subfamily)

EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: MST2/MST2(STK3)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.1 4.5 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 1.3 0.0 1.0
midostaurin Hs Inhibitor Inhibition 1.9 3.0 0.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 2.7 5.0 0.0
K-252a Hs Inhibitor Inhibition 2.9 2.0 1.0
Gö 6976 Hs Inhibitor Inhibition 3.1 2.0 2.0
SB 218078 Hs Inhibitor Inhibition 3.2 10.0 12.0
PKR inhibitor Hs Inhibitor Inhibition 3.4 2.0 1.0
indirubin derivative E804 Hs Inhibitor Inhibition 4.8 4.0 1.0
JAK inhibitor I Hs Inhibitor Inhibition 5.4 14.0 4.0
SU9516 Hs Inhibitor Inhibition 12.2 16.0 3.0
bosutinib Hs Inhibitor Inhibition 13.9
SU11652 Hs Inhibitor Inhibition 16.9 34.0 2.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 19.9 6.0 0.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 20.5 10.0 5.0
Syk inhibitor Hs Inhibitor Inhibition 23.4 27.0 6.0
SU6656 Hs Inhibitor Inhibition 24.3 28.0 22.0
sunitinib Hs Inhibitor Inhibition 24.8
PKR inhibitor, negative control Hs Inhibitor Inhibition 31.6 49.0 2.0
JNJ-7706621 Hs Inhibitor Inhibition 34.3 34.0 4.0
dovitinib Hs Inhibitor Inhibition 34.4
GSK-3 inhibitor X Hs Inhibitor Inhibition 39.5 65.0 18.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 40.9 27.0 7.0
isogranulatimide Hs Inhibitor Inhibition 41.0 68.0 33.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 41.4 56.0 18.0
GF109203X Hs Inhibitor Inhibition 44.2 73.0 17.0
GTP-14564 Hs Inhibitor Inhibition 49.6 101.0 57.0
PKCbeta inhibitor Hs Inhibitor Inhibition 52.0 64.0 13.0
Cdk4 inhibitor Hs Inhibitor Inhibition 55.8 89.0 62.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 58.5 55.0 11.0
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 60.7 46.0 61.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 62.1 68.0 8.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 62.1 66.0 7.0
semaxanib Hs Inhibitor Inhibition 64.0 70.0 15.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 64.7 64.0 9.0
H-89 Hs Inhibitor Inhibition 65.6 115.0 90.0
SP600125 Hs Inhibitor Inhibition 67.2 16.0 10.0
aminopurvalanol A Hs Inhibitor Inhibition 70.0 106.0 60.0
alsterpaullone Hs Inhibitor Inhibition 70.3 71.0 21.0
Gö 6983 Hs Inhibitor Inhibition 72.2 93.0 38.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 73.7 85.0 72.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 74.4 55.0 11.0
Y27632 Hs Inhibitor Inhibition 75.7 105.0 79.0
aloisine A Hs Inhibitor Inhibition 76.6 86.0 45.0
SU11274 Hs Inhibitor Inhibition 78.6 89.0 59.0
wortmannin Hs Inhibitor Inhibition 79.5
tozasertib Hs Inhibitor Inhibition 80.2
PP1 analog II Hs Inhibitor Inhibition 82.0 91.0 29.0
kenpaullone Hs Inhibitor Inhibition 83.2 87.0 28.0
CGP74514A Hs Inhibitor Inhibition 83.9 108.0 70.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 85.0
tofacitinib Hs Inhibitor Inhibition 85.8
PDGF RTK inhibitor Hs Inhibitor Inhibition 86.0 97.0 77.0
aloisine Hs Inhibitor Inhibition 87.0 94.0 68.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 87.0 105.0 71.0
PD 174265 Hs Inhibitor Inhibition 88.0 121.0 91.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 88.3 97.0 96.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 88.4 97.0 78.0
bohemine Hs Inhibitor Inhibition 88.7 111.0 99.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 88.8 101.0 74.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 88.9 117.0 95.0
Cdk1 inhibitor Hs Inhibitor Inhibition 89.1 101.0 62.0
AG 9 Hs Inhibitor Inhibition 89.3 110.0 97.0
JAK3 inhibitor II Hs Inhibitor Inhibition 89.6 97.0 70.0
BPIQ-I Hs Inhibitor Inhibition 89.9 98.0 92.0
fasudil Hs Inhibitor Inhibition 90.0 90.0 95.0
D4476 Hs Inhibitor Inhibition 90.6 114.0 107.0
dasatinib Hs Inhibitor Inhibition 90.6
CGP53353 Hs Inhibitor Inhibition 90.7 100.0 68.0
MNK1 inhibitor Hs Inhibitor Inhibition 90.8 104.0 82.0
purvalanol A Hs Inhibitor Inhibition 90.8 104.0 35.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 91.4 111.0 99.0
vatalanib Hs Inhibitor Inhibition 92.1
PP3 Hs Inhibitor Inhibition 92.3 107.0 93.0
PD 169316 Hs Inhibitor Inhibition 92.5 110.0 99.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 92.6 94.0 91.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 93.0 98.0 76.0
GSK-3beta inhibitor I Hs Inhibitor Inhibition 93.2 98.0 97.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 93.3 98.0 86.0
Cdk/Crk inhibitor Hs Inhibitor Inhibition 93.5 109.0 78.0
BAY 11-7082 Hs Inhibitor Inhibition 93.6 99.0 95.0
gefitinib Hs Inhibitor Inhibition 93.6
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 93.6 110.0 92.0
lapatinib Hs Inhibitor Inhibition 93.7
seliciclib Hs Inhibitor Inhibition 93.8
dorsomorphin Hs Inhibitor Inhibition 93.9 111.0 100.0
nilotinib Hs Inhibitor Inhibition 93.9
VX-702 Hs Inhibitor Inhibition 94.1
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 94.2 89.0 85.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 94.3 42.0 4.0
masitinib Hs Inhibitor Inhibition 94.4
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 94.6 71.0 36.0
tandutinib Hs Inhibitor Inhibition 94.7
MK2a inhibitor Hs Inhibitor Inhibition 94.8 98.0 73.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 94.9 102.0 83.0
erlotinib Hs Inhibitor Inhibition 94.9
herbimycin A Hs Inhibitor Inhibition 95.0 110.0 102.0
AG 112 Hs Inhibitor Inhibition 95.2 108.0 100.0
pazopanib Hs Inhibitor Inhibition 95.4
mubritinib Hs Inhibitor Inhibition 95.5
AG 1296 Hs Inhibitor Inhibition 95.7 120.0 100.0
aurora kinase inhibitor III Hs Inhibitor Inhibition 96.0 99.0 64.5
fascaplysin Hs Inhibitor Inhibition 96.7 101.0 100.0
sorafenib Hs Inhibitor Inhibition 96.9
STO609 Hs Inhibitor Inhibition 97.1 103.0 81.0
PD98059 Hs Inhibitor Inhibition 97.1 97.0 98.0
AGL 2043 Hs Inhibitor Inhibition 97.1 107.0 87.0
vandetanib Hs Inhibitor Inhibition 97.5
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 97.5 117.0 97.0
MEK inhibitor I Hs Inhibitor Inhibition 97.6 97.0 93.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 97.6 111.0 81.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 97.7 110.0 94.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 97.7 109.0 92.0
Lck inhibitor Hs Inhibitor Inhibition 97.7 91.0 11.0
imatinib Hs Inhibitor Inhibition 97.9
Syk inhibitor II Hs Inhibitor Inhibition 98.0 103.0 77.0
MEK inhibitor II Hs Inhibitor Inhibition 98.2 99.0 83.0
GW-2580 Hs Inhibitor Inhibition 98.4 105.0 96.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 98.5 107.0 104.0
KN-62 Hs Inhibitor Inhibition 98.8 99.0 83.0
JNK inhibitor V Hs Inhibitor Inhibition 98.9 97.0 56.0
Akt inhibitor IV Hs Inhibitor Inhibition 98.9 109.0 71.0
DNA-PK inhibitor III Hs Inhibitor Inhibition 98.9 121.0 116.0
AG 1295 Hs Inhibitor Inhibition 98.9 88.0 95.0
PQ401 Hs Inhibitor Inhibition 98.9 109.0 80.0
NU-7026 Hs Inhibitor Inhibition 99.1 113.0 111.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 99.5 103.0 71.0
Flt-3 inhibitor Hs Inhibitor Inhibition 99.6 105.0 91.0
PD 158780 Hs Inhibitor Inhibition 99.9 103.0 88.0
DMBI Hs Inhibitor Inhibition 100.0 108.0 60.0
JNK inhibitor VIII Hs Inhibitor Inhibition 100.0 108.0 100.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 100.2 106.0 102.0
DNA-PK inhibitor V Hs Inhibitor Inhibition 100.2 108.0 95.0
ERK inhibitor III Hs Inhibitor Inhibition 100.4 110.0 108.0
KU-55933 Hs Inhibitor Inhibition 100.6 92.0 93.0
KN-93 Hs Inhibitor Inhibition 100.7 99.0 78.0
triciribine Hs Inhibitor Inhibition 101.3 105.0 104.0
chelerythrine Hs Inhibitor Inhibition 101.9 107.0 94.0
Ro-32-0432 Hs Inhibitor Inhibition 101.9
EGFR inhibitor Hs Inhibitor Inhibition 101.9 106.0 65.0
ERK inhibitor II Hs Inhibitor Inhibition 102.0 79.0 91.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 102.1 88.0 88.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 102.1 120.0 93.0
SB203580 Hs Inhibitor Inhibition 102.2 104.0 93.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 102.3 109.0 92.0
LY 303511 Hs Inhibitor Inhibition 102.3 95.0 104.0
Akt inhibitor VIII Hs Inhibitor Inhibition 102.8 106.0 80.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 102.9 103.0 99.0
SB220025 Hs Inhibitor Inhibition 103.5 87.0 93.0
Cdk4 inhibitor II Hs Inhibitor Inhibition 103.5 96.0 93.0
SC-68376 Hs Inhibitor Inhibition 103.8 102.0 96.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 103.8 102.0 72.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 104.1 96.0 100.0
SB 202474 Hs Inhibitor Inhibition 104.5 118.0 97.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 104.9 100.0 72.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 105.0 109.0 100.0
SB202190 Hs Inhibitor Inhibition 105.2 108.0 90.0
PI-103 Hs Inhibitor Inhibition 105.2 120.0 101.0
purvalanol A Hs Inhibitor Inhibition 105.3 104.0 35.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 105.9 103.0 94.0
Akt inhibitor X Hs Inhibitor Inhibition 106.3 118.0 112.0
AG 490 Hs Inhibitor Inhibition 106.6 107.0 98.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 106.9 98.0 71.0
Syk inhibitor III Hs Inhibitor Inhibition 106.9 104.0 91.0
AG 1024 Hs Inhibitor Inhibition 107.5 107.0 86.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 107.6 109.0 92.0
TWS119 Hs Inhibitor Inhibition 108.7 99.0 69.0
Chk2 inhibitor II Hs Inhibitor Inhibition 109.3 100.0 74.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 110.3 39.0 15.0
JNK inhibitor IX Hs Inhibitor Inhibition 111.4 95.0 91.0
SKF-86002 Hs Inhibitor Inhibition 111.4 99.0 93.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 111.7 103.0 81.0
SKI II Hs Inhibitor Inhibition 114.4 101.0 76.0
IC261 Hs Inhibitor Inhibition 115.5 102.0 91.0
Src kinase inhibitor I Hs Inhibitor Inhibition 121.2 96.0 80.0
AG1478 Hs Inhibitor Inhibition 124.3 100.0 74.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 125.5 76.0 80.0
LY 294002 Hs Inhibitor Inhibition 103.0 98.0

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]