SB-242235

SB-242235 is an inhibitor of p38α MAPK (IC₅₀ = 0.019 µM).¹ It is selective for p38α MAPK over a panel of 10 kinases, including ERK2, JNK1, EGFR, and C-RAF (IC₅₀s = >10 µM 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 µM, 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

WARNING This product is not for human or veterinary use.

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 activity. Bioorg. 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 cultures. Osteoarthritis Cartilage 8(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 mice. J. 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 arthritis. Arthritis Rheum. 43(1), 175-183 (2000).