Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].

Topoisomerase IIα-IN-4 (0-50 μM; 72 h) shows antiproliferative activities against cancer cells [1]. Topoisomerase IIα-IN-4 shows high inhibitory activity and subtypeselectivity against TopoIIα and β with IC 50 s of 3.8 and 10.1 μM, respectively [1]. Topoisomerase IIα-IN-4 (0.3 μM; 4 h) is a non-intercalative TopoIIα catalytic inhibitor [1]. Topoisomerase IIα-IN-4 (0.5-1 μM; 48 h) induces cell apoptosis [1]. Topoisomerase IIα-IN-4 (0.5-1 μM; 24 h) induces cell-cycle arrest [1]. Cell Proliferation Assay [1] Cell Line: HeLa, HCT-116, MDA-MB231, HepG2, A549, CCL-226, BEAS-2B and HL-7702 cell lines Concentration: 0-50 μM Incubation Time: 72 hours Result: Inhibited HeLa, HCT-116, MDA-MB 231, HepG2, A549, CCL-226, BEAS-2B and HL-7702 cells with IC 50 s of 0.1, 0.2, 0.3, 0.2, 0.3, 0.3, ＞50, 31.9 and 16.7 μM, respectively. Western Blot Analysis [1] Cell Line: HepG-2 cell line Concentration: 0.3 μM Incubation Time: 4 hours Result: Showed no effect on the level of phospho-histone H2AX. Apoptosis Analysis [1] Cell Line: 0.5-1 μM Concentration: 0.3 μM Incubation Time: 48 hours Result: Increased the total numbers of early and late apoptotic cells from 6.0% to 70.6% at the concentration of 1 μM.

Topoisomerase IIα-IN-4 (500 mg/kg; p.o. twice at the first day) shows no acute toxicity in vivo [1]. Animal Model: C57BL/6 mice [1] Dosage: 500 mg/kg Administration: Oral gavage; 500 mg/kg twice at the first day Result: Exerted lower toxicity in this established test and caused no significant difference of body weight of mice.