ksq-4279

KSQ-4279 (USP1-IN-1) is a dual USP1/PARP inhibitor, a potent and selective PARP inhibitor with anti-cancer activity, used for research in non-small cell lung cancer and various other cancers.

KSQ-4279 (gentisate) (Compound Formula I) serves as an effective inhibitor of USP1 and a selective inhibitor of PARP1. This compound shows promise for use in cancer research.

USP1-IN-9 (Compound 1m) is a reversible and non-competitive inhibitor of ubiquitin-specific protease (USP1) with an IC50 value of 8.8 nM. It is synthesized based on the structures of ML323 and KSQ-4279 as a pyrido[2,3-d]pyrimidin-7(8H)-one derivative. USP1-IN-9 exhibits excellent inhibition of USP1/UAF and demonstrates strong antiproliferative effects on breast cancer cells. When combined with the PARP inhibitor olaparib, USP1-IN-9 enhances the cytotoxic effect on MDA-MB-436/OP cells. USP1-IN-9 holds potential for research in the field of cancer.