iRucaparib-AP6 is a novel and potent PARP1 degrader based on PROTAC (Proteolysis-targeting chimera) technology. It is composed of Rucaparib as the warhead to bind PARP1 and pomalidomide to recruit the E3 ligase. iRucaparib-AP6 blocks the enzymatic activity of PARP1 in vitro, and PARP1-mediated poly-ADP-ribosylation signaling in intact cells. This strategy mimics PARP1 genetic depletion, which enables the pharmacological decoupling of PARP1 inhibition from PARP1 trapping. Finally, by depleting PARP1, iRucaparib-AP6 protects muscle cells and primary cardiomyocytes from DNA-damage-induced energy crisis and cell death.

纯度：≥98%

CAS：2410557-00-3