Topoisomerase II inhibitor 3 (Compound 6 h ) 是吖啶酮衍生物，也是一种 Type II DNA 拓扑异构酶 (topo II) 的抑制剂,具有topo IIα/β抑制剂作用，topo IIα 亚型的 IC50 值为 0.17 μM， topo IIβ 亚型的 IC50 值为 0.23 μM，还可引起明显的 DNA 损伤，并通过触发线粒体膜电位的丧失诱导细胞凋亡。

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 IC 50 is 0.17 μM for topo IIα and the value of IC 50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced 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.

99140-25-7

C18H20N4O4

356.38

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years