PARP/EZH2-IN-2 (compound 12e) functions as a dual inhibitor targeting both PARP1 and EZH2, with IC50 values of 6.89 and 27.34 nM, respectively. This compound exhibits anticancer activity without toxicity to normal cells, achieving synthetic lethality indirectly by increasing PARP1 sensitivity through EZH2 inhibition, and inducing cell death by modulating excessive autophagy.

EZH2:27.34 ± 1 nM, PARP1:6.89 ± 0.7 nM