Topoisomerase II inhibitor 3

Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

IC50: 0.17 μM (topo IIα); IC50: 0.23 μM (topo IIβ)[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 IC50 is 0.17 μM for topo IIα and the value of IC50 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 (IC50: 0.42 μM), A549 cells (IC50: 1.10 μM), KG1 cells (IC50: 0.15 μM) and H9C2 cells (IC50 >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.

[1]. Zhi-Ying Li, et al. Structural optimizations and bioevaluation of N-substituted acridone derivatives as strong topoisomerase II inhibitors. Bioorg Chem. 2022 Feb;119:105543.