General description

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. The solid form of this compound (Cat. No. 220486) is also available.

Legal Information

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

Other Notes

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

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

Supplied as a 25 mM (5 mg/550 µL) solution of Chk2 Inhibitor II (Cat. No. 220486) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Warning

Toxicity: Irritant (B)