Table 2 Kinase selectivity profiling of SB-747651A, H89 and Ro 31-8220

Inhibitors were profiled in vitro against a panel of kinases as described in the Materials and methods section. The final concentration of the inhibitors in the assay was 1 μM, and results are expressed as the percentage activity remaining relative to control reactions without inhibitor. Kinases are ordered by their ability to inhibit MSK1. Results with less than 15% of activity remaining are in bold typeface. For definitions of kinase abbreviations, see http://www.kinase-screen.mrc.ac.uk/kinase-panel.htm/.

SB-747651AH89Ro 31-8220
KinaseSpeciesGenBank® accession number[ATP] (μM)Activity remaining (%)Range (n=2)Activity remaining (%)Range (n=2)Activity remaining (%)Range (n=2)
MSK1HumanAF074393205025010
PRK2HumanS7554855014131
RSK1HumanNM_002953.3506132241
S6K1HumanNM_00316120609120
ROCK-IIRatU38481207191703
PKBαHumanNM_00162650150241131
PIM-1HumanNM_0026482018391362
RSK2HumanNM_00458650193701010
PKBβHumanNM_00274250242491131
PIM-3HumanQ86V8620261010513244
MELKHumanNM_0147915037664124210
PKAHumanBC000479538250211
PKCζHumanNM_00273020522872460
IGF-1RHumanNM_00087555613882413
IRRHumanNM_0142155576886230
DYRK1AHumanNM_130437.25059183141
ERK8HumanAY065978560855531
PKCαHumanNM_005030563293640
AMPKHumanBC0274645631767143913
SGK1HumanNM_0056272064264861
PKCγHumanNM_00273920655537392
MARK3HumanU642055671093118037
PAK6HumanQ9NQU5206798927811
MLK1HumanNM_033141206829106643
CHK2HumanNM_00719420685580346
TTKHumanNM_003318206910750352
GSK3βHumanL33801569299511
Aurora BHumanAF533878507057310314
BRSK1HumanNM_03243020717858381
TAK1HumanNM_0031885720872377
FGF-R1HumanM346412073490104024
PKD1HumanNM_00273720746803385
STK33HumanBC031231.150744423102
MNK2HumanAF237775507425122331077
GCKHumanBC04786520744939150
PRAKHumanAF03243720759841920
MKK1RabbitZ3016357519511280
MKK2HumanNM_03066257511836245
MINK1HumanNM_0157165077082591
p38δ MAPKHumanY1048757716903848
JNK1HumanL26318207728915763
MARK2HumanNM_004954207829046123
MAPKAPK2HumanNM_0329602078158412758
CLK2HumanNM_003993.2578395110
CDK2–cyclin AHumanNM_0017982079685341
SYKHumanAAH01645.120792963695
MST4HumanNM_016542207912884211
VEGFRHumanNM_002019.32080189451
NUAK1HumanNM_01484020802181191
MEKK1HumanXM_0420662081159098413
DAPK1HumanNM_004938.25819945435
CK1HumanNM_00189320820897945
MNK1HumanAB00040950831944944
TAO1HumanNM_020791208312872348
EPH-B1HumanNM_00444120837976832
CK2HumanNM_00189558449359315
IRAK4HumanBC013316.12084121047404
BTKHumanNP_00052.150843988403
ZAP70HumanNM_001079584161073733
PIM2HumanU7773558410917143
YES1HumanNM_005433208559924110
SrcHumanNM_005417.3508581001895
PAK5HumanQ9P28620861110411755
HER4HumanNM_00523558628711404
EPH-B2HumanNM_004442208751005571
BRSK2HumanAF53387850878682378
HIPK1HumanNM_19826820876961232
IKKβHumanXM_0324915881944843
RIPK2HumanNM_0038212088149211894
TrkAHumanNM_001007792.1208820107171
IKKϵHumanNM_014002508861056757
NEK6HumanNM_0143975089189108512
PDK1HumanX8059050898847304
JNK3HumanNM_002753208998711918
CAMK1HumanNM_003656508939013386
DYRK3HumanAY5906955905614181
EPH-B3HumanNM_00444320904103139121
Aurora AHumanNM_03243020905883932
MARK1HumanAF15484520901958757
CHK1HumanAF016582209010707123
HIPK2HumanAF32659259061005141
JAK2HumanNP_004963.159151040554
NEK2aHumanNM_00249750911952854
PAK4HumanO960135913921492
CSKHumanNM_00438320926942958
EF2KHumanAAH32665592010915795
ABLRatTissue purified50929944880
ERK1HumanBC0139925926954851
EPH-A2HumanNM_00443150931975574
IRHumanNM_000208.220943102191010
EPH-A4HumanNM_00443850943977533
PAK2HumanNM_002577209439758413
ERK2HumanNM_00274520950944888
SRPK1HumanNM_00313750951905291
p38β MAPKHumanY1444020962873924
MST2HumanU60206209614912163
MLK3HumanNM_0024192096993971
CAMKKβHumanNM_1534992096711419131
MAPKAPK3HumanNM_0046352097410449220
PHKHumanNM_00261320971092181
BRKHumanNP_00052.150978886848
DYRK2HumanNM_00358350978994868
p38α MAPKHumanL35264509741031858
LKB1HumanNP_000446209861223775
MKK6HumanNM_002758509959015742
SmMLCKHumanNM_005965509931011110
PLK1HumanNM_002744510189739513
MPSK1HumanCR4076755010189961031
ASK1HumanNM_004217201016951901
TIE2HumanBC035514.12010261171897
MARK4HumanAK075272501034988723
TBK1HumanNM_01325450105119129282
JNK2HumanL31951201055961796
LckMouseX035335010689815566
EPH-B4HumanNP_004435.35011213890744
HIPK3HumanNM_00573420120141087475
p38γ MAPKHumanY104885128538715916
  • The calculated Km for ATP in these assays results in a poor signal-to-noise ratio, so assays are performed with an ATP concentration above the Km.