Doramapimod (285983-48-4) potently and selectively inhibits p38 MAPK by simultaneously binding to the ATP-binding domain and an allosteric site.1 (IC50=18 nM). Displays anti-inflammatory activity2 but differential effects on inflammatory genes3. Cell permeable.
1) Pargellis et al. (2002), Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site; Nat. Struct. Biol., 9 268
2) Branger et al. (2002), Anti-inflammatory effects of a p38 mitogen-activated protein kinase inhibitor during human endotoxemia; J. Immunol., 168 4070
3) Joos et al. (2010), Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in primary, interleukin-1 beta-stimulated human chondrocytesl; Br. J. Pharmacol., 160 1252