| Bioactivity | PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability[1]. |
| Invitro | PARP-2-IN-3 (Compound 12) (24 h) shows cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively[1].PARP-2-IN-3 (6.05 μM; 24 h) arrests cell cycle at G2/M phase, and induces apoptosis and necrosis in MCF-7 cells[1].PARP-2-IN-3 fills the space inside the PARP-2 pocket in a manner similar to Olaparib (HY-10162)[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| Name | PARP-2-IN-3 |
| Formula | C20H20ClN3O3 |
| Molar Mass | 385.84 |
| 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]. El-Ghobashy NM, et al. Synthesis, biological evaluation, and molecular modeling studies of new benzoxazole derivatives as PARP-2 inhibitors targeting breast cancer. Sci Rep. 2022 Sep 28;12(1):16246. |