Description
A potent, selective, orally active p38alpha/p38beta inhibitor with IC50 of 11.2/36.5nM respectively, with no effect on p38gamma and delta isoforms (IC50>1uM); displays no activity against a panel of 100 protein kinases, including JNK2, EGFR, Akt and Pim; inhibits LPS- or PHA-induced production of proinflammatory cytokines, including TNFalpha, IL-1beta, and IL-6 at low concentrations (LPS/TNFalpha, IC50=0.45nM; PHA/TNFalpha, IC50=0.40nM) in human PBMCs, also inhibits TNFalpha- and IL-1 beta-induced production of IL-6, PGE (2), and MMP-3 in human synovial stromal cells; potently inhibits TNF production in whole blood (IC50=12nM) and effectively inhibits TNFalpha production induced by LPS in rats with long-acting anti-inflammatory effect