Topoisomerase I inhibitor 2 (ZML-8) 是一种高度选择性的DNA topoisomerase I(Top1) 抑制剂。Topoisomerase I inhibitor 2 抑制Top1活性，导致 DNA 损伤。Topoisomerase I inhibitor 2 还能够阻断 G2/M 期，诱导细胞凋亡 (apoptosis)，具有抗肿瘤作用。
| 生物活性 | TopoisomeraseI inhibitor 2 (ZML-8) is a highly selective inhibitor ofDNAtopoisomeraseI(Top1).TopoisomeraseI inhibitor 2 inhibitsTop1activity and results DNA damage.TopoisomeraseI inhibitor 2 blocks G2/M phase and inducesapoptosis, exhibits anti-tumor effect[1]. |
| IC50& Target | Topoisomerase I 0.58 μM (IC50) |
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体外研究
(In Vitro) | Topoisomerase I inhibitor 2 (ZML-8) (24 hours) exhibits strong inhibition with an IC50value of 0.58 μM towards HepG2 and selective activity with SI values (selectivity index) of 55.70% between HepG2 and normal human liver cell line L-02[1].
Topoisomerase I inhibitor 2 (1.25, 2.5 μM, 48 hours) inhibits tumor cells proliferation by decreasing anti-apoptotic expression of Bcl-2 and enhancing caspase-dependent apoptosis[1].
Topoisomerase I inhibitor 2 (1.25, 2.5 μM, 48 hours) decreases Top1 specific activity and results in DNA damage by causing supercoiled DNA[1].
Cell Cycle Analysis[1] | Cell Line: | HepG2 cells | | Concentration: | 2.5 μM | | Incubation Time: | 24 hours | | Result: | Arrested the cell cycle in G2/M phase in a dose-dependent manner. |
Cell Proliferation Assay[1] | Cell Line: | HepG2 cells | | Concentration: | 0.625, 1.25, 2.5 μM | | Incubation Time: | 48 hours | | Result: | Inhibited tumor cells proliferation by inducing cell apoptosis in a dose-dependent manner, the apoptosis rate was 65.0% and 77.6%, respectively. |
Western Blot Analysis[1] | Cell Line: | HepG2 cells | | Concentration: | 0.625, 1.25, 2.5 μM | | Incubation Time: | 48 hours | | Result: | Decreased anti-apoptotic expression of Bcl-2 at 2.5 μM significantly and increased the expression of pro-apoptotic protein Bax, Bad, and p53. And also significantly enhanced caspase- dependent apoptosis and activated Cleaved caspase-3 in a dose-dependent manner. |
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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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