506121

p38 MAP Kinase Inhibitor III

The p38 MAP Kinase Inhibitor III, also referenced under CAS 581098-48-8, controls the biological activity of p38 MAP Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): p38 MAP Kinase Inhibitor III, ML3403, (RS)-{4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl}-(1-phenylethyl)amine]
• Empirical Formula (Hill Notation): C₂₃H₂₁FN₄S
• CAS Number: 581098-48-8
• Molecular Weight: 404.50
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C23H21FN4S/c1-15(16-6-4-3-5-7-16)26-20-14-18(12-13-25-20)22-21(27-23(28-22)29-2)17-8-10-19(24)11-9-17/h3-15H,1-2H3,(H,25,26)(H,27,28)
• InChI key: VXPWQNBKEIVYIS-UHFFFAOYSA-N

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
p38 MAP kinase

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°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: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable