PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer.
PARP-1-IN-3 (compound 13f; 48 h) has potent anticancer activity with IC50 values of 0.30, 2.83, 33.69, and 486.87 μM for HCT116, DLD-1, SW480, and NCM460 cells, respectively[1].PARP-1-IN-3 (0.3-3 μM; 24-48 h) inhibits colony formation and migration of HCT116 cells[1].PARP-1-IN-3 (0.3-3 μM; 48 h) induces accumulation of DNA double-strand breaks in HCT116 cells[1].PARP-1-IN-3 (0.3-7.5 μM; 48-72 h) arrests cell cycle at G2/M phase, reduces mitochondrial membrane potential and ultimately induce apoptosis in HCT116 cells[1].
References:
[1]. Lu G, et, al. Discovery of novel benzamide derivatives bearing benzamidophenyl and phenylacetamidophenyl scaffolds as potential antitumor agents via targeting PARP-1. Eur J Med Chem. 2023 May 5;251:115243.