| Bioactivity | PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy[1]. |
| Invitro | PARP/EZH2-IN-2 (compound 12e) 对 MDA-MB-231 细胞 (IC50=2.84 μM) 和 BT-549 细胞 (IC50=0.91 μM) 显示出最佳的细胞毒性，对正常乳腺细胞系没有毒性[1]。 0 --> PARP/EZH2-IN-2 相关抗体: |
| In Vivo | PARP/EZH2-IN-2 (compound 12e) (20-50 mg/kg, 腹腔注射) 表现出良好的抗肿瘤活性，优于 Niraparib (HY-10619) + GSK126 (HY-13470)[1]。 Animal Model: |
| Name | PARP/EZH2-IN-2 |
| Formula | C33H31N7O3 |
| Molar Mass | 573.64 |
| 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]. Li X, et al. Dual target PARP1/EZH2 inhibitors inducing excessive autophagy and producing synthetic lethality for triple-negative breast cancer therapy. Eur J Med Chem. 2023 Dec 17;265:116054. |