1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis Bcl-2 Family
  3. Topoisomerase II inhibitor 23

Topoisomerase II inhibitor 23 是一种强效的拓扑异构酶 II (topoisomerase II) 抑制剂, IC50 值为 0.94 μM。与阿霉素 (HY-15142A) (IC50 值为 3.08 μM) 相比,Topoisomerase II inhibitor 23 在 MCF-7、HepG2 和 HCT116 细胞中表现出高选择性和卓越的细胞毒性作用。Topoisomerase II inhibitor 23 诱导细胞周期停滞在 G1 期,从而抑制细胞增殖。Topoisomerase II inhibitor 23 通过上调促凋亡蛋白 Bax 和下调抗凋亡蛋白 Bcl-2 水平诱导细胞凋亡 (apoptosis)。

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Topoisomerase II inhibitor 23 Chemical Structure

Topoisomerase II inhibitor 23 Chemical Structure

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  • 生物活性

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  • 参考文献

生物活性

Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level[1].

体外研究
(In Vitro)

Topoisomerase II inhibitor 23 (Compound, IId) 对 MCF-7、HepG2 和 HCT116 细胞展现出优秀的细胞毒性作用,IC50 值分别为 24.52 μM,28.92 μM 和54.38 μM[1]

Topoisomerase II inhibitor 23 对 MCF-7、HepG2 和 HCT116 细胞具有高选择性,在人细胞系 BJ 细胞上的选择性指数分别为 3.8、3.3 和 1.7[1]

Topoisomerase II inhibitor 23 (24.52 μM, 24 h) 可使细胞生长停滞在 G1 期,从而抑制 MCF-7 细胞的增殖[1]

Topoisomerase II inhibitor 23 (24.52 μM, 24 h) 通过上调 MCF-7 细胞中促凋亡蛋白 Bax 水平和下调抗凋亡蛋白 Bcl-2 水平诱导细胞凋亡[1]

Topoisomerase II inhibitor 23 显示出强大的拓扑异构酶 II 抑制活性 (IC50 值为 0.94μM),高于阿霉素 (HY-15142A) (IC50 值为 3.08 μM)[1]

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

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 24.52 μM
Incubation Time: 24 h
Result: Increased the percentage of cells at G0/G1 to 84.13 % in comparison to the control (61.09%).
Induced a lower reduction in the cell percentage of cells at S phase (30.56 %) than Doxorubicin (HY-15142A) (12.32 %).
Decreased population of cells at G2/M phase (3.55 %) than the control (9.27 %).

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 24.52 μM
Incubation Time: 24 h
Result: Increased annexin-V positive apoptotic cells at the early and late apoptotic stages and necrosis percentage.
Significantly up-regulated the pro-apoptotic Bax expression level by 6.96 fold and down-regulated the anti-apoptotic Bcl-2 expression level by 0.23 fold.
分子量

531.46

Formula

C28H23BrN2O2S

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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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    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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产品名称:
Topoisomerase II inhibitor 23
目录号:
HY-174404
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