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Description: SB239063 (SB-239063) is a novel, highly potent, orally bioactive and selective p38 MAPKalpha/beta inhibitor with potential anti-inflammatory activity. It inhibits p38 MAPKalpha/beta with an IC50 of 44 nM, and shows no/little activity against the p38 MAPK gamma- and delta-isoforms. SB 239063 displays > 220-fold selectivity for p38 MAPK over ERK, JNK1 and other kinases; and is around 3-fold more selective than SB 203580. In LPS (lipopolysaccharide)-stimulated human peripheral blood monocytes, SB 239063 inhibited interleukin-1 and tumor necrosis factor-alpha production (IC(50) values = 0.12 and 0.35 microM, respectively). SB 239063 may be useful for the treatment of asthma and other inflammatory disorders.
References: J Pharmacol Exp Ther. 2000 Apr; 293(1):281-8; Eur J Pharmacol. 2008 Sep 11; 592(1-3):55-61.
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