Chk2 Inhibitor II-CAS 516480-79-8-Calbiochem

C₂₀H₁₄ClN₃O₂

363.80

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.

Primary Target
Chk2
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
Target K_i: 37 nM inhibiting Chk2
Reversible: yes
Cell permeable: yes
Product competes with ATP.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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

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

100

≥95% (HPLC)

solid

15 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

pale yellow

DMSO: 5 mg/mL

ambient

2-8℃

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3