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Beschreibung

A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 380 nM for p38alpha). Shown to effectively suppress LPS-induced cytokine release in vitro (IC50 = 160 nM for TNF-alpha release and 39 nM for IL-1beta release, human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-alpha release in mice). Exhibits reduced inhibitory activity against cytochrome P450-2D6 compared to SB 203580 (Cat. No 559389) and is better suited for use in animal models., A cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC50 = 0.38 µ,M for p38alpha). Shown to effectively suppresses LPS-induced cytokine release both in vitro (IC50 = 0.16 and 0.039 µ,M for TNF-alpha and IL-1beta release, respectively, in human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-alpha release in mouse). When compared with SB 203580 (Cat. No. 559389 and 559398), it exhibits reduced inhibitory activity against cytochrome P450-2D6 isoform and, therefore, is better suited for in vivo use. A 10 mM (1 mg/247 µ,l) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506148) in DMSO is also available.