Chemical Name:4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]
phenol
Biological Activity:
A highly selective, potent and
cell-permeable inhibitor of p38 MAP kinase. Binds within the ATP pocket of the
active kinase (Kd = 38 nM, as measured in recombinant human p38),
and selectively inhibits the p38α
and β isoforms (IC50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38β2
respectively).
Jianget al (1996) Characterization
of the structure and function of a new mitogen-activated protein kinase (p38β). J.Biol.Chem. 271
17920. Frantzet al (1998) The activation of p38
mitogen-activated protein kinase determines the efficiency of ATP competition
for pyridinylimidazole inhibitor binding. Biochemistry 37 13846. Nemoto
et al (1998) Induction of apoptosis by SB 202190 through inhibition
of p38β mitogen-activated
protein kinase. J.Biol.Chem. 273 16415. Davies et al
(2000) Specificity and mechanism of action of some commonly used protein kinase
inhibitors. Biochem.J. 351 95.