PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2/M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.

HCT116 cells:0.30 μM, NCM460 cells:486.87 μM, PARP1:0.25 nM, PARP2:2.34 nM, SW480 cells:33.69 μM, DLD-1 cells:2.83 μM

PARP-1-IN-3 (compound 13f) demonstrates effective anticancer activity with IC50 values of 0.30 μM, 2.83 μM, 33.69 μM, and 486.87 μM against HCT116, DLD-1, SW480, and NCM460 cells, respectively, following a 48-hour treatment[1]. In HCT116 cells, PARP-1-IN-3 (0.3-3 μM) inhibits colony formation and migration over 24-48 hours[1]. A 48-hour treatment with PARP-1-IN-3 (0.3-3 μM) induces the accumulation of DNA double-strand breaks in HCT116 cells[1]. Treatment with PARP-1-IN-3 (0.3-7.5 μM) for 48-72 hours results in cell cycle arrest at the G2/M phase, reduced mitochondrial membrane potential, and apoptosis in HCT116 cells[1].