TABLE 1

Effect of SB-505124 on the activities of protein kinases in vitro Protein kinases were assayed with 10 μ M SB-505124 in the presence of 0.1 mM ATP. Activities are given as the mean of duplicate determinations relative to control incubations with DMSO vehicle.

Protein Kinase Kinase Activity
% control
AMPK 97
CDK2/cyclin A 97
Chk1 101
CK2 98
CSK 100
GSK3β 97
JNK1 103
lck 96
MAPK2 82
MAPKAP-K1β 95
MAPKAP-K2 81
MKK1 94
MSK1 98
p70 S6K 118
PDK1 95
Phos. kinase 63
PI3-kinase 93
PKA 119
PKBα 95
PKCα 127
PRAK 96
ROKα 95
p38 MAPKα 15a
p38 MAPKβ 70
p38 MAPKγ 97
p38 MAPKδ 98
SGK 77
  • AMPK, adenosine monophosphate-activated protein kinase; CDK, cyclin dependent kinase; Chk1, checkpoint kinase 1; CK2, casein kinase 2; CSK, c-src tyrosine kinase; GSK3β, glycogen synthase kinase 3β; lck, lymphocyte-specific protein kinase; MAPK2, mitogen activated protein kinase 2; MAPKAP-K1β, MAPK-activated protein kinase-1β; MAPKAP-K2, MAPK-activated protein kinase-2; MKK1, mitogen activated protein kinase kinase 1; MSK, mitogen- and stress-activated kinase; p70 S6K, 70-kDa S6 protein kinase; PDK1, phosphoinositide-dependent protein kinase1; PI3K, phosphoinositide 3-kinase; PK, protein kinase; PRAK, p38 regulated/activated protein kinase; ROK, Rho kinase; SGK, serum- and glucocorticoid-inducible kinase.

  • a p38 MAPK α was inhibited with 10 μM SB-505124