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Topoisomerase IIα-IN-4

Topoisomerase IIα-IN-4

产品编号 T61431

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].

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Topoisomerase IIα-IN-4
Topoisomerase IIα-IN-4, CAS N/A
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 10-14周
50 mg ¥ 13,800 10-14周
100 mg ¥ 17,500 10-14周
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Topoisomerase IIα-IN-4 (T61431)
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产品描述 Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].
体外活性 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 IC 50 s 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]. 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 IC 50 s 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.
体内活性 Topoisomerase IIα-IN-4 (500 mg/kg; p.o. twice at the first day) shows no acute toxicity in vivo [1]. 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
分子式 C25H21NO2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Topoisomerase IIα-IN-4 Inhibitor inhibitor inhibit

 

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