Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC 50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.