SB 242235

193746-75-7

C19H20FN5O

DMSO : >= 48 mg/mL (135.83 mM)

MAPK/ERK Pathway

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC₅₀ of 1.0?uM in primary human chondrocytes^[1]. IC50 & Target: IC50: 1.0?uM (p38 MAPK, primary human chondrocytes)^[1] In Vitro: SB 242235 (0-10?uM) dose-dependently inhibits the activation of MAPKAP K2 with an IC₅₀ of 1.0 uM in human chondrocytes stimulated with IL-1beta^[1].
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate^[1].
In Vivo: SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation^[2].
SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2^[2].
SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey^[3].