Chk2 Inhibitor for cell activation

A cell-permeable, potent, and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2; IC₅₀ = 15 nM; Ki = 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.

N/A

516480-79-8

363.8

Biochemicals

2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide

C₂₀H₁₄CIN₃O₂

Pale yellow solid

N/A

No

Yes

≥98% by HPLC

DMSO (10 mg/ml)

-20°C

gel pack

12 months

Protect from air and moisture

cell

For cells, cell lines and tissues in culture till half confluency.Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.