Topoisomerase I inhibitor 2
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.
For research use only. We do not sell to patients.
- CAS No.: 2588211-44-1
- Formula: C18H15NO3
- Molecular Weight:293.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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Topoisomerase I 0.58 μM (IC50) |
In Vitro
Topoisomerase I inhibitor 2 (ZML-8) (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:2.5 μM
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Incubation Time:24 hours
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Result:Arrested the cell cycle in G2/M phase in a dose-dependent manner.
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Cell Line:HepG2 cells
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Concentration:0.625, 1.25, 2.5 μM
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Incubation Time:48 hours
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Result:Inhibited tumor cells proliferation by inducing cell apoptosis in a dose-dependent manner, the apoptosis rate was 65.0% and 77.6%, respectively.
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Cell Line:HepG2 cells
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Concentration:0.625, 1.25, 2.5 μM
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Incubation Time:48 hours
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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.
Chemical Information
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CAS No. 2588211-44-1
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Molecular Weight 293.32
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Formula C18H15NO3
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SMILES
COC1=C(C=C2N=C3COC4=C(C3=CC2=C1)C=CC=C4)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Topoisomerase I inhibitor 2 Related Classifications
HY-143265 Related Classifications
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