Adezmapimod (SB-203580) hydrochloride

Description: SB203580 (also known as RWJ 64809) is a novel and potent p38 mitogen-activated protein kinase inhibitor (p38MAPK inhibitor) with IC50 of 0.3-0.5 uM in THP-1 cells, it is 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 uM. SB203580 suppresses the development of endometriosis by down-regulating proinflammatory cytokines and proteolytic factors in a mouse model. SB203580 is a competitive ATPsite inhibitor of p38MAPK with a selectivity probably determined by nonconserved regions within or near the ATP binding pocket and a Ki of 21 nM.

References: J Biol Chem. 2000 Mar 10; 275(10):7395-402; Br J Pharmacol. 2000 Sep; 131(1):99-107.

Related CAS#: 152121-47-6 (free base)