559396

SB 220025

A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC₅₀ = 60 nM).

• Synonyme(s) : SB 220025, 5-(2-Amino-4-pyrimidinyl)-4-(4-fluorophenyl)-1-(4-piperidinlyl)imidazole, p38 MAP Kinase Inhibitor XIV
• Formule empirique (notation de Hill): C₁₈H₁₉FN₆
• Numéro CAS: 165806-53-1
• Poids moléculaire : 338.38
• Code UNSPSC : 12352202
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Puissance: 60 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: white to pale yellow
• Solubilité: DMSO: 22 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C18H19FN6/c19-13-3-1-12(2-4-13)16-17(15-7-10-22-18(20)24-15)25(11-23-16)14-5-8-21-9-6-14/h1-4,7,10-11,14,21H,5-6,8-9H2,(H2,20,22,24)
• Clé InChI: VSPFURGQAYMVAN-UHFFFAOYSA-N

Description

Description générale

A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC₅₀ = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits over 2000-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1000-fold over EGFR. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

A potent and specific inhibitor of human p38 mitogen-activated protein (MAP) kinase (IC₅₀ = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits >2500-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1600-fold over EGFRK. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.

Actions biochimiques/physiologiques

Primary Target
P38MAPK

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Jackson, J.R., et al. 1998. J. Pharmacol. Exp. Ther.284, 687.
Wang, Z., et al. 1998. Structure6, 1117.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1