Table 2

Activity of D000 against a panel of protein kinases

The selectivity of D000 (5 μM) was tested against a panel of 29 protein kinases by in vitro kinase assay (KinaseProfiler™, Upstate) in the presence of 100 μM ATP. SD = standard deviation.

KinaseActivity (% of control) ± SD
Akt/PKBα102 ± 5.9
AMPK78 ± 6.0
CDK2/cyclin A101 ± 8.5
CHK198 ± 2.8
CK190 ± 1.3
CK296 ± 0.2
CSK97 ± 8.2
DYRK1a112 ± 1.5
GSK3β90 ± 0.0
JNK/SAPK1c97 ± 11
Lck105 ± 5.0
MAPK2/ERK2113 ± 0.3
MAPKAP-K1a132 ± 4.0
MAPKAP-K2107 ± 7.0
MKK1110 ± 6.2
MSK186 ± 10
PDK192 ± 2.0
Phosphorylase kinase111 ± 5.0
PKA121 ± 12
PKCα104 ± 2.7
PP2a102 ± 0.0
PRAK93 ± 4.0
ROCK-II106 ± 8.3
S6K197 ± 2.8
SAPK2a/p38107 ± 11
SAPK2b/p38β2107 ± 2.1
SAPK3/p38γ114 ± 6.6
SAPK4/p38δ104 ± 6.4
SGK115 ± 12