Biochem/physiol Actions

Chk2 Inhibitor II is a checkpoint kinase 2 inhibitor, which controls the p53 response to DNA breaks induced by radiation, leading to apoptosis. Protection of T-cells from apoptosis implies use as an adjuvant for radiation therapy in cancer. IC₅₀ = 15 nM; K_i = 37 nM. Chk2 Inhibitor II shows 1000-fold greater selectivity for the Chk2 serine/threonine kinase than for the Cdk1/B and CK1 kinases (for which IC₅₀ = 12 µM and 17 µM, respectively). Chk2 Inhibitor II weakly inhibits a panel of 31 other kinases (﹤25% inhibition at a concentration of 10 µM and prevents apoptosis of human CD4+ and CD8+ T-cells subjected to ionizing radiation (EC₅₀ = 3 µM and 7.6 µM, respectively).

Features and Benefits

This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Packaging

5, 25 mg in glass bottle