1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis
  3. Topoisomerase II inhibitor 3

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。

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Topoisomerase II inhibitor 3 Chemical Structure

Topoisomerase II inhibitor 3 Chemical Structure

CAS No. : 99140-25-7

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  • 生物活性

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生物活性

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].

IC50 & Target

IC50: 0.17 μM (topo IIα); IC50: 0.23 μM (topo IIβ)[1]

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

356.38

Formula

C18H20N4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Topoisomerase II inhibitor 3
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