InSolution p38 MAP Kinase Inhibitor III - Calbiochem (C15-1304-385)

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
p38 MAP kinase

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

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).

Other Notes

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

Legal Information

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

Molecular Weight: 404.50. Empirical Formula: C₂₃H₂₁FN₄S. Quality Level: 100. Assay: ≥. 98% (HPLC). form: liquid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. shipped in: wet ice. storage temp.: 2-8°C. Storage Class Code: 10 - Combustible liquids. WGK: WGK 1. Flash Point(F): 188.6 °F - (Dimethylsulfoxide). Flash Point(C): 87 °C - (Dimethylsulfoxide).