220486

Chk2 Inhibitor II

Chk2 Inhibitor II, BML-277, CAS 516480-79-8 is a cell-permeable, potent, reversible, ATP-competitive inhibitor of Chk2 (IC₅₀ = 15 nM).

• Synonyme(s) : Chk2 Inhibitor II, 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide
• Formule empirique (notation de Hill): C₂₀H₁₄ClN₃O₂
• Numéro CAS: 516480-79-8
• Poids moléculaire : 363.80
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Puissance: 15 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: pale yellow
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C20H14ClN3O2/c21-14-4-8-16(9-5-14)26-15-6-1-12(2-7-15)20-23-17-10-3-13(19(22)25)11-18(17)24-20/h1-11H,(H2,22,25)(H,23,24)
• Clé InChI: UXGJAOIJSROTTN-UHFFFAOYSA-N

Description

Description générale

A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC₅₀ of 15 nM and a K_i of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC₅₀ = 12 M and 17 M, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 M), including Chk1. Shown to rescue both peripheral CD4⁺ and CD8⁺ T-cells from γ-irradiation-induced apoptosis with an EC₅₀ of 3 M and 7.6 M, respectively. Also available as a 25 mM solution in DMSO (Cat. No. 220491).

A cell-permeable, potent, reversible and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2; IC₅₀ = 15 nM; K_i = 37 nM). Displays ~1,000-fold greater selectivity for Chk2 compared to Cdk1/cyclin B and CK1 (IC₅₀ = 12 µM and 17 µM, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 µM), including Chk1. Shown to rescue both peripheral CD4⁺ and CD8⁺ T-cells from γ-irradiation-induced apoptosis with an EC₅₀ of 3 µM and 7.6 µM, respectively.

Actions biochimiques/physiologiques

Cell permeable: yes

Ki = 37 nM inhibiting Chk2.EC50 = 3 µM and 7.6 µM in rescuing both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis

Primary Target
Chk2

Product competes with ATP.

Reversible: yes

Target K_i: 37 nM inhibiting Chk2

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 6 months at -20°C.

Autres remarques

Arienti, K. L., et al. 2005. J. Med. Chem.48, 1873.

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 3