CCT241533 hydrochloride is a selective CHK2 inhibitor (IC50=3 nM, Ki=1.16 nM) with minimal cross-reactivity against kinases at 1 μM. It inhibits CHK2 autophosphorylation at S516, blocks CHK2 activity in tumor cells, and potentiates PARP inhibitor cytotoxicity. Its GI50 values in HT-29, HeLa, MCF-7 are 1.7, 2.2, 5.1 μM respectively.
