2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase Apoptosis
  4. Topoisomerase IIα-IN-4

Topoisomerase IIα-IN-4 (F2) 是非嵌入性、ATP 竞争性的 人 DNA 拓扑异构酶 II 抑制剂，对 TopoIIα 和 TopoIIβ 的 IC50 值分别为 3.8 和 10.1 μM。Topoisomerase IIα-IN-4 在 HepG2 细胞中具有诱导凋亡和细胞周期阻滞的作用。Topoisomerase IIα-IN-4 对人类癌细胞株具有较强的抗肿瘤活性，可用于癌症的研究。

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Topoisomerase IIα-IN-4 Chemical Structure

Topoisomerase IIα-IN-4 Chemical Structure

CAS No. : 2860554-26-1

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Topoisomerase IIα-IN-4 相关抗体

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer[1].

IC50 & Target

topoisomerase II alpha

3.8 μM (IC50)

topoisomerase II beta

10.1 μM (IC50)

体外研究
(In Vitro)

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 IC50s 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].

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

Topoisomerase IIα-IN-4 相关抗体:

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 IC50s 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.
体内研究
(In Vivo)

Topoisomerase IIα-IN-4 (500 mg/kg; p.o. twice at the first day) shows no acute toxicity in vivo[1].

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

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.
分子量

367.44

Formula

C25H21NO2
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

Topoisomerase IIα-IN-4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Topoisomerase IIα-IN-42860554-26-1TopoisomeraseApoptosis1,2-diphenyletheneVP-16non-intercalativeATP-competitivecatalyticanti-tumorantiproliferativeHepG2apoptosiscell cycleInhibitorinhibitorinhibit

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