p38 MAP Kinase Inhibitor III-CAS 581098-48-8-Calbiochem

C₂₃H₂₁FN₄S

404.50

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.
A cell-permeable, potent, selective, reversible, 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.

Cell permeable: yes
Product competes with ATP.
Primary Target
p38 MAP kinase
Target IC₅₀: 0.38 µM for p38 MAP kinase α; 0.16 and 0.039 µM in suppressing LPS-induced TNF-α and IL-1β release, respectively, in human PBMC
Reversible: yes

Toxicity: Carcinogenic / Teratogenic (D)

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

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

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

yellow

DMSO: 5 mg/mL

ambient

2-8℃

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1