SB-242235 is an inhibitor of p38α MAPK (IC50 = 0.019 ?M).1 It is selective for p38α MAPK over a panel of 10 kinases, including ERK2, JNK1, EGFR, and C-RAF (IC50s = >10 ?M for all). SB-242235 inhibits IL-1α-induced production of nitric oxide (NO) in bovine articular cartilage explants but not IL-1β-induced production of NO in human articular cartilage explants (IC50s = ~1 and >20 ?M, respectively).2 It inhibits increases in epidermal COX-2 levels and erythema in mice exposed to UVB irradiation when administered at a dose of 100 mg/kg.3 SB-242235 (10, 30, and 60 mg/kg) reduces paw edema in a rat model of adjuvant-induced arthritis.4
1.Adams, J.L., Boehm, J.C., Gallagher, T.F., et al.Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activityBioorg. Med. Chem. Lett.11(21)2867-2870(2001) 2.Badger, A.M., Roshak, A.K., Cook, M.N., et al.Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte culturesOsteoarthritis Cartilage8(6)434-443(2000) 3.Kim, A.L., Labasi, J.M., Zhu, Y., et al.Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless miceJ. Invest. Dermatol.124(6)1318-1325(2005) 4.Badger, A.M., Griswold, D.E., Kapadia, R., et al.Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritisArthritis Rheum.43(1)175-183(2000)