| Bioactivity | PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells[1]. |
| Invitro | PARP1-IN-12 (compound 20e) (0.1, 0.3, 1 µM; 48 h) exhibits activities of antiproliferation and selectively killing BRCA-deficient cells, can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells in a concentration-dependent manner[1].PARP1-IN-12 (10 µM, 48 h) enhances the protein levels of phosphorylated Chk1[1].PARP1-IN-12 (1, 3, 10 µM; 48 h) activats cell cycle checkpoints, then induces G2/M arrest in BRCA-deficient cells and (1, 5, 10 µM; 96 h) also induces MDA-MB-436 cells apoptosis in a concentration-dependent manner[1]. Cell Proliferation Assay[1] Cell Line: |
| Name | PARP1-IN-12 |
| Formula | C43H56FN5O5 |
| Molar Mass | 741.93 |
| 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]. Kayumov M, et al. Design, synthesis and pharmacological evaluation of new PARP1 inhibitors by merging pharmacophores of olaparib and the natural product alantolactone. Eur J Med Chem. 2022 Jun 28;240:114574. |