Bioactivity | 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[1]. |
Invitro | PARP-1-IN-3 (compound 13f; 48 h) 具有有效的抗癌活性,对 HCT116、DLD-1、SW480 和 NCM460 细胞的 IC50 值分别为 0.30、2.83、33.69 和 486.87 μM[1].PARP-1-IN-3 (0.3-3 μM; 24-48 h) 抑制 HCT116 细胞的集落形成和迁移[1]。PARP-1-IN-3 (0.3-3 μM; 48 h) 诱导 HCT116 细胞中 DNA 双链断裂的积累[1].PARP-1-IN-3 (0.3-7.5 μM; 48-72 h) 使细胞周期停滞在 G2/M 期,降低线粒体膜电位并最终诱导 HCT116 细胞凋亡[1]。 Apoptosis Analysis[1] Cell Line: |
Name | PARP-1-IN-3 |
Formula | C21H17BrN2O3 |
Molar Mass | 425.28 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |