p38 MAP Kinase Inhibitor III

(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC₅₀ = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC₅₀s = 0.37 and 0.044 μM, respectively).

p38 MAP Kinase Inhibitor III (compound 7h) is a p38 MAPK inhibitor with an 50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with 50 values of 0.37 μM and 0.044 μM, respectively[1].

A cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC₅₀ = 0.38 μM for p38α). Shown to effectively suppresses LPS-induced cytokine release both in vitro (IC₅₀ = 0.16 and 0.039 μM for TNF-α and IL-1β release, respectively, in human PBMC) and in vivo (ED₅₀ = 1.33 mg/kg for TNF-α 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 μl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506148) in DMSO is also available.

Cell permeable: yes

p38 MAP kinase: 0.9 μM (IC₅₀)

[1] Stefan A Laufer, et al. Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J Med Chem. 2003 Jul 17;46(15):3230-44. DOI:10.1021/jm030766k