Chemical Name:4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-i
midazol-4-yl]pyridine
Biological Activity:
Selective inhibitor of p38 mitogen-activated protein kinase (IC50
values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK,
GSK3b and PKBα. Shown to inhibit interleukin-2-induced T-cell
proliferation, cyclooxygenase-1 and -2, and thromboxane synthase. Also
available as a water-soluble salt (Cat. No. 1402).
Cuenda et al (1995) SB 203580 is a specific inhibitor of a MAP kinase
homologue which is stimulated by cellular stresses and interleukin-1. FEBS
Lett. 364 229. Saklatvalaet al (1996) Role for p38
mitogen-activated protein kinase in platelet aggregation caused by collagen on
a thromboxane analogue. J.Biol.Chem. 271 6586. Borsch-Haubold et
al (1998) Direct inhibition of cyclooxygenase-1 and -2 by the kinase
inhibitors SB 203580 and PD 98059. J.Biol.Chem. 273 28766. Davieset al (2000) Specificity and mechanism of action of some commonly used
protein kinase inhibitors. Biochem.J. 351 95.