Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα/β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1].

Topoisomerase II inhibitor 3 (Compound 6 h ) has function as a strong topo IIα/β inhibitor, causeS obvious DNA damage, and induces apoptosis by triggering the loss of mitochondrial membrane potential. Topoisomerase II inhibitor 3 (Compound 6 h ) is a topo IIα/β dual inhibitor with the value of IC 50 is 0.17 μM for topo IIα and the value of IC 50 is 0.23 μM for topo IIβ subtypesl. Topoisomerase II inhibitor 3 (Compound 6 h ) also can induce the formation of DSBs in a does-dependent manner [1]. Cell Proliferation Assay [1] Cell Line: Human breast cancer MDA-MB-231 cells; human lung cancer A549; human acute myelogenous leukemia KG1 cells; rat myocardial H9C2 cells Concentration: 100 μM Incubation Time: 12 h Result: Exerted the most potent anti-proliferative activity in MDA-MB-231 cells (IC 50 : 0.42 μM), A549 cells (IC 50 : 1.10 μM), KG1 cells (IC 50 : 0.15 μM) and H9C2 cells (IC 50 >20 μM). Apoptosis Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 0.5-10 μM Incubation Time: 24 h Result: Caused obvious loss of mitochondrial membrane potential (MMP) in MDA-MB-231 cells.