ribosomal protein S6 kinase A1 (RSK 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: Rsk1/RSK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition -6.0 1.0 2.0
midostaurin Hs Inhibitor Inhibition 0.4 0.0 1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 0.9 10.0 2.0
SB 218078 Hs Inhibitor Inhibition 1.6 13.0 7.0
staurosporine Hs Inhibitor Inhibition 3.5 3.5 1.0
GF109203X Hs Inhibitor Inhibition 4.7 15.0 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 5.3 4.0 3.0
Ro-32-0432 Hs Inhibitor Inhibition 5.9
PKCbeta inhibitor Hs Inhibitor Inhibition 7.5 8.0 1.0
indirubin derivative E804 Hs Inhibitor Inhibition 8.9 18.0 12.0
Gö 6976 Hs Inhibitor Inhibition 9.7 7.0 4.0
Syk inhibitor Hs Inhibitor Inhibition 12.7 9.0 6.0
SU11652 Hs Inhibitor Inhibition 13.1 11.0 2.0
Gö 6983 Hs Inhibitor Inhibition 16.0 6.0 1.0
PKR inhibitor Hs Inhibitor Inhibition 20.4 28.0 4.0
dovitinib Hs Inhibitor Inhibition 22.2
sunitinib Hs Inhibitor Inhibition 28.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 30.1 40.0 9.0
isogranulatimide Hs Inhibitor Inhibition 31.1 58.0 43.0
aminopurvalanol A Hs Inhibitor Inhibition 37.2 32.0 6.0
JAK inhibitor I Hs Inhibitor Inhibition 38.6 65.0 55.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 39.6 40.0 6.0
JNJ-7706621 Hs Inhibitor Inhibition 42.1 28.0 8.0
semaxanib Hs Inhibitor Inhibition 44.1 51.0 11.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 47.2 72.0 73.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 48.4 94.0 29.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 52.0 85.0 33.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 53.1 109.0 103.0
SU11274 Hs Inhibitor Inhibition 54.4 93.0 51.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 57.1 58.0 7.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 57.6 22.0 3.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 58.0 51.0 15.0
Cdk4 inhibitor Hs Inhibitor Inhibition 58.4 63.0 49.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 59.9 45.0 24.0
SU6656 Hs Inhibitor Inhibition 68.1 95.0 95.0
H-89 Hs Inhibitor Inhibition 68.4 53.0 24.0
SP600125 Hs Inhibitor Inhibition 68.4 86.0 64.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 69.0 105.0 59.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 69.1 50.0 22.0
SU9516 Hs Inhibitor Inhibition 69.6 60.0 17.0
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 70.4 84.0 81.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 71.1 125.0 65.0
herbimycin A Hs Inhibitor Inhibition 76.8 115.0 84.0
purvalanol A Hs Inhibitor Inhibition 77.3 77.0 19.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 77.6 117.0 82.0
PQ401 Hs Inhibitor Inhibition 77.8 125.0 116.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 78.0 121.0 66.0
JAK3 inhibitor II Hs Inhibitor Inhibition 78.2 92.0 45.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 78.2 120.0 76.0
DMBI Hs Inhibitor Inhibition 78.4 66.0 34.0
fascaplysin Hs Inhibitor Inhibition 78.6 97.0 116.0
JNK inhibitor V Hs Inhibitor Inhibition 79.0 102.0 53.0
dorsomorphin Hs Inhibitor Inhibition 79.2 95.0 74.0
PP3 Hs Inhibitor Inhibition 79.5 105.0 88.0
PI-103 Hs Inhibitor Inhibition 79.5 141.0 98.0
JNK inhibitor VIII Hs Inhibitor Inhibition 79.9 103.0 100.0
bosutinib Hs Inhibitor Inhibition 80.4
PI 3-Kg inhibitor Hs Inhibitor Inhibition 80.7 112.0 83.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 82.0 93.0 118.0
MNK1 inhibitor Hs Inhibitor Inhibition 82.2 106.0 64.0
aloisine A Hs Inhibitor Inhibition 82.6 89.0 104.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 82.8 100.0 72.0
IC261 Hs Inhibitor Inhibition 82.8 102.0 101.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 84.1 112.0 79.0
PD 169316 Hs Inhibitor Inhibition 84.3 101.0 104.0
Syk inhibitor II Hs Inhibitor Inhibition 84.3 116.0 59.0
bohemine Hs Inhibitor Inhibition 84.9 102.0 82.0
Y27632 Hs Inhibitor Inhibition 84.9 90.0 48.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 85.7 120.0 95.0
JNK inhibitor IX Hs Inhibitor Inhibition 86.1 113.0 94.0
ERK inhibitor III Hs Inhibitor Inhibition 86.3 125.0 107.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 86.9 90.0 59.0
Flt-3 inhibitor Hs Inhibitor Inhibition 87.0 99.0 103.0
AG1478 Hs Inhibitor Inhibition 87.3 90.0 69.0
PP1 analog II Hs Inhibitor Inhibition 87.8 107.0 65.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 88.1 117.0 108.0
AG 1296 Hs Inhibitor Inhibition 88.4 107.0 57.0
Chk2 inhibitor II Hs Inhibitor Inhibition 88.6 91.0 67.0
PD 174265 Hs Inhibitor Inhibition 88.7 119.0 84.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 88.7 40.0 42.0
fasudil Hs Inhibitor Inhibition 89.2 84.0 47.0
alsterpaullone Hs Inhibitor Inhibition 89.7 106.0 91.0
aloisine Hs Inhibitor Inhibition 89.8 122.0 109.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 90.2 106.0 83.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 90.4 116.0 63.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 90.5 110.0 89.0
kenpaullone Hs Inhibitor Inhibition 90.8 78.0 77.0
tofacitinib Hs Inhibitor Inhibition 90.9
PD 158780 Hs Inhibitor Inhibition 90.9 115.0 59.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 91.3 129.0 99.0
Cdk/Crk inhibitor Hs Inhibitor Inhibition 91.3 105.0 56.0
wortmannin Hs Inhibitor Inhibition 91.3
BAY 11-7082 Hs Inhibitor Inhibition 91.6 94.0 121.0
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 92.0 129.0 85.0
NU-7026 Hs Inhibitor Inhibition 92.0 108.0 97.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 92.3
DNA-PK inhibitor III Hs Inhibitor Inhibition 92.4 121.0 110.0
GW-2580 Hs Inhibitor Inhibition 92.7 131.0 109.0
PD98059 Hs Inhibitor Inhibition 92.7 91.0 81.0
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 92.7 130.0 94.0
pazopanib Hs Inhibitor Inhibition 92.8
aurora kinase inhibitor III Hs Inhibitor Inhibition 92.8 72.5 38.5
JNK inhibitor, negative control Hs Inhibitor Inhibition 93.7 114.0 93.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 93.8 117.0 67.0
AG 112 Hs Inhibitor Inhibition 93.8 94.0 78.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 94.0 98.0 106.0
Lck inhibitor Hs Inhibitor Inhibition 94.2 123.0 39.0
Cdk4 inhibitor II Hs Inhibitor Inhibition 94.6 116.0 106.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 94.6 2.0 1.0
tandutinib Hs Inhibitor Inhibition 94.8
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 94.8 51.0 15.0
EGFR inhibitor Hs Inhibitor Inhibition 95.1 105.0 79.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 95.1 113.0 101.0
ERK inhibitor II Hs Inhibitor Inhibition 95.1 108.0 93.0
Syk inhibitor III Hs Inhibitor Inhibition 95.7 137.0 106.0
dasatinib Hs Inhibitor Inhibition 96.2
DNA-PK inhibitor V Hs Inhibitor Inhibition 96.2 96.0 85.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 96.4 113.0 106.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 96.4 136.0 109.0
MEK inhibitor II Hs Inhibitor Inhibition 96.6 120.0 131.0
SB220025 Hs Inhibitor Inhibition 96.7 105.0 91.0
masitinib Hs Inhibitor Inhibition 97.2
gefitinib Hs Inhibitor Inhibition 97.3
PDGF RTK inhibitor Hs Inhibitor Inhibition 97.3 96.0 81.0
LY 294002 Hs Inhibitor Inhibition 97.3 138.0 99.0
Akt inhibitor X Hs Inhibitor Inhibition 97.5 110.0 117.0
Src kinase inhibitor I Hs Inhibitor Inhibition 97.6 122.0 78.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 97.6 113.0 118.0
GSK-3beta inhibitor I Hs Inhibitor Inhibition 97.6 118.0 125.0
erlotinib Hs Inhibitor Inhibition 97.6
KU-55933 Hs Inhibitor Inhibition 97.6 87.0 94.0
CGP53353 Hs Inhibitor Inhibition 97.7 87.0 91.0
SKI II Hs Inhibitor Inhibition 97.7 113.0 103.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 97.9 118.0 87.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 97.9 113.0 61.0
mubritinib Hs Inhibitor Inhibition 97.9
SB202190 Hs Inhibitor Inhibition 98.1 117.0 83.0
AG 9 Hs Inhibitor Inhibition 98.3 135.0 104.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 98.6 55.0 46.0
AG 1295 Hs Inhibitor Inhibition 99.2 95.0 86.0
AGL 2043 Hs Inhibitor Inhibition 99.4 115.0 89.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 99.4 82.0 74.0
SB203580 Hs Inhibitor Inhibition 99.9 86.0 80.0
GTP-14564 Hs Inhibitor Inhibition 100.0 97.0 58.0
SKF-86002 Hs Inhibitor Inhibition 100.1 73.0 81.0
imatinib Hs Inhibitor Inhibition 100.5
sorafenib Hs Inhibitor Inhibition 100.8
STO609 Hs Inhibitor Inhibition 100.9 103.0 79.0
Akt inhibitor VIII Hs Inhibitor Inhibition 101.0 117.0 84.0
MEK inhibitor I Hs Inhibitor Inhibition 101.1 104.0 115.0
vandetanib Hs Inhibitor Inhibition 102.0
MK2a inhibitor Hs Inhibitor Inhibition 102.1 90.0 89.0
AG 490 Hs Inhibitor Inhibition 102.2 115.0 102.0
D4476 Hs Inhibitor Inhibition 102.3 126.0 102.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 102.4 104.0 78.0
SC-68376 Hs Inhibitor Inhibition 102.6 88.0 97.0
BPIQ-I Hs Inhibitor Inhibition 102.8 97.0 92.0
seliciclib Hs Inhibitor Inhibition 102.9
triciribine Hs Inhibitor Inhibition 102.9 110.0 109.0
tozasertib Hs Inhibitor Inhibition 103.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 103.3 115.0 76.0
nilotinib Hs Inhibitor Inhibition 103.7
chelerythrine Hs Inhibitor Inhibition 103.7 108.0 92.0
AG 1024 Hs Inhibitor Inhibition 103.9 111.0 87.0
Akt inhibitor IV Hs Inhibitor Inhibition 104.0 114.0 84.0
LY 303511 Hs Inhibitor Inhibition 104.1 124.0 96.0
purvalanol A Hs Inhibitor Inhibition 104.3 77.0 19.0
TWS119 Hs Inhibitor Inhibition 104.8 97.0 68.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 105.0 113.0 81.0
lapatinib Hs Inhibitor Inhibition 105.1
Cdk1 inhibitor Hs Inhibitor Inhibition 105.2 106.0 42.0
SB 202474 Hs Inhibitor Inhibition 105.5 105.0 104.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 107.9 58.0 41.0
KN-93 Hs Inhibitor Inhibition 108.2 119.0 103.0
VX-702 Hs Inhibitor Inhibition 108.8
KN-62 Hs Inhibitor Inhibition 108.9 97.0 87.0
vatalanib Hs Inhibitor Inhibition 112.8
CGP74514A Hs Inhibitor Inhibition 67.0 16.0

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]