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^[1].

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.

293.32

C₁₈H₁₅NO₃

2588211-44-1

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

Room temperature in continental US; may vary elsewhere.

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• [1]. Zhou Y, et al. Design and synthesis of Aza-boeravinone derivatives as potential novel topoisomerase I inhibitors. Bioorg Chem. 2022 May. 122:105747.  [Content Brief]