Cayman Chk2 Inhibitor

Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2; IC₅₀ = 13.5 nM). It is selective for Chk2 over Chk1 (IC₅₀ = 220.4 nM). It inhibits Chk2 autophosphorylation at the serine in position 516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 when used at concentrations ranging from 0.1 to 30 µM. Chk2 inhibitor enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation and inhibits cell cycle arrest at the g₂ stage induced by ionizing radiation in 184B5 cells. It also inhibits the production of IL-2 in Jurkat cells stimulated by phorbol 12-myristate 13-acetate (PMA; Item No. ) and the production of TNF-α in LPS-stimulated THP-1 cells (IC₅₀s = 3.5 and 8.2 µM, respectively). Chk2 inhibitor also inhibits the growth of CEM leukemia T cells (GI₅₀ = 1.73 µM).

WARNING This product is not for human or veterinary use.