PARP-2-IN-3 (Compound 12) 是一种有效的PARP-2抑制剂，其IC50为 0.07 μM。 PARP-2-IN-3 诱导癌细胞凋亡 (apoptosis) 和坏死。 PARP-2-IN-3 具有较好的预测药代动力学参数和口服生物利用度。
| 生物活性 | PARP-2-IN-3 (Compound 12) is a potentPARP-2inhibitor with anIC50of 0.07 μM. PARP-2-IN-3 inducesapoptosisand necrosis incancercells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | 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 toOlaparib(HY-10162)[1].
Cell Cytotoxicity Assay[1] | Cell Line: | MDA-MB-231 and MCF-7 | | Concentration: | | | Incubation Time: | 24 h | | Result: | Displayed remarkable cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively. |
Cell Cycle Analysis[1] | Cell Line: | MCF-7 | | Concentration: | 6.05 μM | | Incubation Time: | 24 h | | Result: | The percentage of cells in pre-G1 phase increased from 1.85% to 33.47%, while in G2/M phase increased from 11.84% to 32.04%. The percentage of cells in S phase slightly decreased from 29.95% to 26.18% and in G0/G1 phase decreased from 58.21% to 41.78%. |
Apoptosis Analysis[1] | Cell Line: | MCF-7 | | Concentration: | 6.05 μM | | Incubation Time: | 24 h | | Result: | Induced an early apoptotic effect 22.52% and late apoptotic effect 3.72% in comparison to the untreated negative control MCF-7 cells which induced an early and late apoptotic effect 0.37% and 0.33%, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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