Topoisomerase I inhibitor 2
Modify Date: 2024-01-12 13:00:32
Topoisomerase I inhibitor 2 structure
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Common Name | Topoisomerase I inhibitor 2 | ||
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| CAS Number | 2588211-44-1 | Molecular Weight | 293.32 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C18H15NO3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Topoisomerase I inhibitor 2Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1]. |
| Name | Topoisomerase I inhibitor 2 |
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| Description | Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1]. |
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| Related Catalog | |
| Target |
Topoisomerase I:0.58 μM (IC50) |
| In Vitro | Topoisomerase I inhibitor 2 (24 hours) exhibits strong inhibition with an IC50 value 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. |
| References |
| Molecular Formula | C18H15NO3 |
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| Molecular Weight | 293.32 |