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Medchemexpress LLC Cct241533 hydrochloride | 1431697-96-9 | 98.55% | 478.94 | 50 MG
Supplier: Medchemexpress LLC HY14715B50MG
CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM. It exhibits minimal cross-reactivity against a panel of kinases at 1 μM. X-ray crystallography confirms its binding to CHK2 in the ATP pocket. The compound blocks CHK2 activity in human tumor cell lines in response to DNA damage, significantly enhancing the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of the pS516 CHK2 signal by PARP inhibitor alone is abolished by CCT241533. The cytotoxicity (GI50) in HT-29, HeLa, and MCF-7 cells is 1.7, 2.2, and 5.1 μM, respectively.
- Potent and selective CHK2 inhibitor (IC50=3 nM)
- 63-fold selectivity over CHK1 (IC50=190 nM)
- Low hERG inhibition (IC50=22 μM)
- Blocks CHK2 activity in human tumor cell lines in response to DNA damage
- Enhances cytotoxicity of PARP inhibitors
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