inhibitor of nuclear factor kappa B kinase subunit epsilon (IKK family)

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: nd/IKKe(IKBKE)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.3
K-252a Hs Inhibitor Inhibition 2.4
midostaurin Hs Inhibitor Inhibition 9.9
JAK3 inhibitor VI Hs Inhibitor Inhibition 14.9
Syk inhibitor Hs Inhibitor Inhibition 21.9
SB 218078 Hs Inhibitor Inhibition 23.9
JAK inhibitor I Hs Inhibitor Inhibition 25.4
PKR inhibitor Hs Inhibitor Inhibition 27.6
SU11652 Hs Inhibitor Inhibition 29.4
dovitinib Hs Inhibitor Inhibition 42.9
sunitinib Hs Inhibitor Inhibition 45.6
indirubin derivative E804 Hs Inhibitor Inhibition 45.7
STO609 Hs Inhibitor Inhibition 57.3
GSK-3 inhibitor IX Hs Inhibitor Inhibition 66.3
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 67.1
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 67.2
Gö 6976 Hs Inhibitor Inhibition 69.4
dorsomorphin Hs Inhibitor Inhibition 71.9
semaxanib Hs Inhibitor Inhibition 72.8
SU11274 Hs Inhibitor Inhibition 74.2
indirubin-3'-monoxime Hs Inhibitor Inhibition 75.1
bosutinib Hs Inhibitor Inhibition 75.4
Cdk2 inhibitor IV Hs Inhibitor Inhibition 77.9
Ro-32-0432 Hs Inhibitor Inhibition 78.8
GSK-3 inhibitor X Hs Inhibitor Inhibition 81.4
Flt-3 inhibitor III Hs Inhibitor Inhibition 81.6
Flt-3 inhibitor II Hs Inhibitor Inhibition 81.6
Cdk4 inhibitor Hs Inhibitor Inhibition 83.4
JNK inhibitor VIII Hs Inhibitor Inhibition 83.7
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 84.0
tozasertib Hs Inhibitor Inhibition 84.8
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 85.5
vandetanib Hs Inhibitor Inhibition 85.8
AG 1024 Hs Inhibitor Inhibition 86.8
pazopanib Hs Inhibitor Inhibition 87.0
PKCbeta inhibitor Hs Inhibitor Inhibition 87.0
PD 158780 Hs Inhibitor Inhibition 87.1
erlotinib Hs Inhibitor Inhibition 87.6
SU6656 Hs Inhibitor Inhibition 87.9
VX-702 Hs Inhibitor Inhibition 88.0
LY 303511 Hs Inhibitor Inhibition 88.1
TWS119 Hs Inhibitor Inhibition 88.1
aloisine A Hs Inhibitor Inhibition 88.3
aminopurvalanol A Hs Inhibitor Inhibition 88.4
SP600125 Hs Inhibitor Inhibition 88.9
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 89.2
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 89.2
imatinib Hs Inhibitor Inhibition 89.3
GF109203X Hs Inhibitor Inhibition 89.4
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 89.5
sorafenib Hs Inhibitor Inhibition 89.8
kenpaullone Hs Inhibitor Inhibition 89.8
AGL 2043 Hs Inhibitor Inhibition 89.8
gefitinib Hs Inhibitor Inhibition 89.9
dasatinib Hs Inhibitor Inhibition 90.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 90.0
JNK inhibitor V Hs Inhibitor Inhibition 90.3
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 90.6
IKK-2 inhibitor IV Hs Inhibitor Inhibition 90.8
AG 112 Hs Inhibitor Inhibition 91.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 91.4
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 91.8
Akt inhibitor VIII Hs Inhibitor Inhibition 91.9
JNK inhibitor, negative control Hs Inhibitor Inhibition 92.3
H-89 Hs Inhibitor Inhibition 92.3
SU9516 Hs Inhibitor Inhibition 92.5
KN-62 Hs Inhibitor Inhibition 92.6
JAK3 inhibitor IV Hs Inhibitor Inhibition 93.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 93.3
alsterpaullone Hs Inhibitor Inhibition 93.4
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 93.5
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 93.5
KN-93 Hs Inhibitor Inhibition 93.7
JNK inhibitor IX Hs Inhibitor Inhibition 94.3
nilotinib Hs Inhibitor Inhibition 94.6
JAK3 inhibitor II Hs Inhibitor Inhibition 94.6
Akt inhibitor IV Hs Inhibitor Inhibition 94.7
PKR inhibitor, negative control Hs Inhibitor Inhibition 94.7
mubritinib Hs Inhibitor Inhibition 94.8
tofacitinib Hs Inhibitor Inhibition 94.8
PD 169316 Hs Inhibitor Inhibition 94.9
lapatinib Hs Inhibitor Inhibition 94.9
PD 174265 Hs Inhibitor Inhibition 94.9
Rho kinase inhibitor IV Hs Inhibitor Inhibition 95.0
PD98059 Hs Inhibitor Inhibition 95.1
ERK inhibitor II Hs Inhibitor Inhibition 95.5
Cdk/Crk inhibitor Hs Inhibitor Inhibition 95.6
NF-kB activation inhibitor Hs Inhibitor Inhibition 95.6
vatalanib Hs Inhibitor Inhibition 95.7
Syk inhibitor II Hs Inhibitor Inhibition 95.8
JNJ-7706621 Hs Inhibitor Inhibition 95.9
SKI II Hs Inhibitor Inhibition 95.9
tandutinib Hs Inhibitor Inhibition 96.2
PDGF RTK inhibitor Hs Inhibitor Inhibition 96.2
Rho kinase inhibitor III Hs Inhibitor Inhibition 96.4
GSK-3beta inhibitor I Hs Inhibitor Inhibition 96.4
KU-55933 Hs Inhibitor Inhibition 96.5
GW-2580 Hs Inhibitor Inhibition 96.7
casein kinase II inhibitor III Hs Inhibitor Inhibition 96.8
MEK inhibitor I Hs Inhibitor Inhibition 97.1
masitinib Hs Inhibitor Inhibition 97.2
Lck inhibitor Hs Inhibitor Inhibition 97.4
aurora kinase inhibitor III Hs Inhibitor Inhibition 97.5
seliciclib Hs Inhibitor Inhibition 97.6
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 97.6
Y27632 Hs Inhibitor Inhibition 97.6
EGFR inhibitor Hs Inhibitor Inhibition 97.7
wortmannin Hs Inhibitor Inhibition 98.0
SB203580 Hs Inhibitor Inhibition 98.0
Cdk1 inhibitor Hs Inhibitor Inhibition 98.0
MK2a inhibitor Hs Inhibitor Inhibition 98.2
DMBI Hs Inhibitor Inhibition 98.2
PP1 analog II Hs Inhibitor Inhibition 98.3
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 98.3
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 98.3
BPIQ-I Hs Inhibitor Inhibition 98.7
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 98.7
PI-103 Hs Inhibitor Inhibition 98.8
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 98.9
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 98.9
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 98.9
AG 1296 Hs Inhibitor Inhibition 98.9
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 99.0
purvalanol A Hs Inhibitor Inhibition 99.2
purvalanol A Hs Inhibitor Inhibition 99.4
Cdk1/5 inhibitor Hs Inhibitor Inhibition 99.4
SB220025 Hs Inhibitor Inhibition 99.5
CGP74514A Hs Inhibitor Inhibition 99.5
PI 3-Kg inhibitor Hs Inhibitor Inhibition 99.5
MEK inhibitor II Hs Inhibitor Inhibition 99.6
D4476 Hs Inhibitor Inhibition 99.7
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 99.7
SB 202474 Hs Inhibitor Inhibition 99.8
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 99.8
Gö 6983 Hs Inhibitor Inhibition 100.0
MNK1 inhibitor Hs Inhibitor Inhibition 100.0
triciribine Hs Inhibitor Inhibition 100.0
CGP53353 Hs Inhibitor Inhibition 100.1
LY 294002 Hs Inhibitor Inhibition 100.1
PP3 Hs Inhibitor Inhibition 100.2
aloisine Hs Inhibitor Inhibition 100.3
NU-7026 Hs Inhibitor Inhibition 100.6
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 100.6
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 100.7
IC261 Hs Inhibitor Inhibition 100.8
SB202190 Hs Inhibitor Inhibition 100.8
Cdk2 inhibitor III Hs Inhibitor Inhibition 100.9
chelerythrine Hs Inhibitor Inhibition 101.0
ERK inhibitor III Hs Inhibitor Inhibition 101.0
fasudil Hs Inhibitor Inhibition 101.0
AG 1295 Hs Inhibitor Inhibition 101.1
AG1478 Hs Inhibitor Inhibition 101.2
GTP-14564 Hs Inhibitor Inhibition 101.2
DNA-PK inhibitor V Hs Inhibitor Inhibition 101.3
SKF-86002 Hs Inhibitor Inhibition 101.3
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 101.4
BAY 11-7082 Hs Inhibitor Inhibition 101.4
Src kinase inhibitor I Hs Inhibitor Inhibition 101.4
GSK-3beta inhibitor II Hs Inhibitor Inhibition 101.5
Cdk4 inhibitor III Hs Inhibitor Inhibition 101.6
MEK1/2 inhibitor Hs Inhibitor Inhibition 102.2
Akt inhibitor X Hs Inhibitor Inhibition 102.2
SC-68376 Hs Inhibitor Inhibition 102.4
bohemine Hs Inhibitor Inhibition 102.4
AG 9 Hs Inhibitor Inhibition 102.8
isogranulatimide Hs Inhibitor Inhibition 102.9
herbimycin A Hs Inhibitor Inhibition 103.0
Chk2 inhibitor II Hs Inhibitor Inhibition 103.3
bisindolylmaleimide IV Hs Inhibitor Inhibition 103.4
Syk inhibitor III Hs Inhibitor Inhibition 103.7
fascaplysin Hs Inhibitor Inhibition 103.7
Cdk4 inhibitor II Hs Inhibitor Inhibition 103.8
DNA-PK inhibitor III Hs Inhibitor Inhibition 105.4
AG 490 Hs Inhibitor Inhibition 105.5
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 105.9
Flt-3 inhibitor Hs Inhibitor Inhibition 106.1
PQ401 Hs Inhibitor Inhibition 106.7
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 107.3

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]