Chk2 Inhibitor

Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2; IC₅₀ = 13.5 nM).¹ 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. 10008014) and the production of TNF-α in LPS-stimulated THP-1 cells (IC₅₀s = 3.5 and 8.2 µM, respectively).² 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.

1. Nguyen, T.N.T., Saleem, R.S.Z., Luderer, M.J., et al. Radioprotection by hymenialdisine-derived checkpoint kinase 2 inhibitors. ACS Chem. Biol. 7(1), 172-184 (2012).

2. Sharma, V., Lansdell, T.A., Jin, G., et al. Inhibition of cytokine production by hymenialdisine derivatives. J. Med. Chem. 47(14), 3700-3703 (2004).