Biochem/physiol Actions

Primary TargetP38MAPK

General description

A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC₅₀ = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits over 2000-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1000-fold over EGFR. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.Please note that the molecular weight for this compound is batch-specific due to variable water content.

A potent and specific inhibitor of human p38 mitogen-activated protein (MAP) kinase (IC₅₀ = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits >2500-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1600-fold over EGFRK. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Jackson, J.R., et al. 1998. J. Pharmacol. Exp. Ther.284, 687.Wang, Z., et al. 1998. Structure6, 1117.

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)