1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis Caspase
  3. 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.

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Topoisomerase I inhibitor 2 Chemical Structure

Topoisomerase I inhibitor 2 Chemical Structure

CAS No. : 2588211-44-1

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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].

IC50 & Target

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.

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.
Molecular Weight

293.32

Formula

C18H15NO3

CAS No.
SMILES

COC1=C(C=C2N=C3COC4=C(C3=CC2=C1)C=CC=C4)OC

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Topoisomerase I inhibitor 2 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Topoisomerase I inhibitor 2
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HY-143265
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