506148

p38 MAP Kinase Inhibitor III

InSolution, ≥98%

• Synonym(s): InSolution p38 MAP Kinase Inhibitor III
• Empirical Formula (Hill Notation): C₂₃H₂₁FN₄S
• Molecular Weight: 404.50
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point(F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Flash Point(C): 87 °C - closed cup - (Dimethylsulfoxide)