InSolution p38 MAP Kinase Inhibitor III

Biochem/physiol Actions

Target IC₅₀: 0.38 µM for p38α; 0.16 and 0.039 µM in suppressing LPS-induced TNF-α and IL-1β release, respectively, in human PBMC; ED50 = 1.33 mg/kg in suppressing LPS-induced TNF-α release in mouse

Reversible: yes

Product competes with ATP.

Primary Targetp38 MAP kinase

Cell permeable: yes

General description

A cell-permeable, potent, selective, and ATP-competitive inhibitor of p38 MAP kinase (IC₅₀ = 380 nM for p38α). Shown to effectively suppress LPS-induced cytokine release in vitro (IC₅₀ = 160 nM for TNF-α release and 39 nM for IL-1β release, human PBMC) and in vivo (ED₅₀ = 1.33 mg/kg for TNF-α 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.

Legal Information

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

Other Notes

Laufer, S.A., et al. 2003. J. Med. Chem.46, 3230.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

A 10 mM (1 mg/247 µl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506121) in DMSO.

Reconstitution

Following initial use, aliquot and refrigerate (4°C).

Warning

Toxicity: Standard Handling (A)