1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  2. Topoisomerase Reactive Oxygen Species (ROS) Apoptosis MDM-2/p53 Caspase Bcl-2 Family
  3. Topo I/II-IN-3

Topo I/II-IN-3 是一种拓扑异构酶 I/II (topoisomerase I/II) 双重抑制剂,Topo IIC50 为 8.99 μM,Topo IIIC50 为 26.92 μM。Topo I/II-IN-3 可诱导 DNA 损伤、升高细胞内的 ROS 水平、激活线粒体凋亡 (apoptosis) 通路、诱导癌细胞产生细胞毒性。Topo I/II-IN-3 上调细胞中 γ-H2AX 的表达,上调 p53、活化的 caspase-9Bax 及活化的 caspase-3,同时下调 Bcl-2 的表达Topo I/II-IN-3 可用于乳腺癌、肝癌、胃癌的相关研究。

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Topo I/II-IN-3

Topo I/II-IN-3 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC50 of 8.99 μM against Topo I and an IC50 of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of γ-H2AX, p53, activated caspase-9, Bax and activated caspase-3, while downregulating the expression of Bcl-2. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer[1].

IC50 & Target[1]

Topoisomerase I

8.99 ()

Topoisomerase II

26.92 ()

Caspase-9

 

Caspase-3

 

Bax

 

体外研究
(In Vitro)

Topo I/II-IN-3 (Compound A6) (0.6-22.1 μM; 48 h) 可强效抑制 MCF-7、MDA-MB-231、HepG2 和 SGC-7901 癌细胞的增殖,IC50 分别为 0.6、12.6、3.4、5.4 μM,且对正常 HEK-293 细胞的细胞毒性较低 (IC50 = 22.1 μM)[1]
Topo I/II-IN-3 (1.56-100 μM; 30 min) 可阻断 DNA 松弛作用和 kDNA 解连环作用,IC50 分别为为 8.99、26.92 μM[1]
Topo I/II-IN-3 (0.3-1.2 μM; 24 h) 可在 MCF-7 细胞中诱导剂量依赖性 DNA 损伤,上调细胞中 γ-H2AX 的表达,上调 p53、活化的 caspase-9、Bax 及活化的 caspase-3,同时下调 Bcl-2[1]
Topo I/II-IN-3 (0.25-1 μM; 24-48 h) 可强效抑制 MCF-7 细胞的长期增殖,抑制 MCF-7 细胞的迁移[1]
Topo I/II-IN-3 (0.3-1.2 μM; 24 h) 可在 MCF-7 细胞中诱导剂量依赖性的 G2/M 期阻滞,诱导细胞凋亡,升高细胞内的 ROS 水平,降低线粒体膜电位[1]

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

Western Blot Analysis[1]

Cell Line: MCF-7
Concentration: 0, 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
Result: Markedly upregulated γ-H2AX protein expression in a dose-dependent manner, confirming induction of DNA double-strand breaks.\nDose-dependently upregulated expression of p53, cleaved caspase-9, Bax, and cleaved caspase-3, while downregulating Bcl-2 expression.

Cell Proliferation Assay[1]

Cell Line: MCF-7
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 48 h
Result: Significantly impaired clonogenicity in a dose-dependent manner; at 1 μM, colony formation fell to below 20% of the control.

Cell Migration Assay [1]

Cell Line: MCF-7
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 24 h, 48 h
Result: Significantly reduced cell migration in a dose-dependent manner; at 1 μM, anti-migratory effects were comparable to positive controls CPT and VP-16.

Cell Cycle Analysis[1]

Cell Line: MCF-7
Concentration: 0, 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
Result: Induced dose-dependent G2/M phase arrest, with increasing proportions of cells in G2/M phase and decreasing proportions in G0/G1 phase as concentrations rose.

Apoptosis Analysis[1]

Cell Line: MCF-7
Concentration: 0, 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
Result: Significantly induced apoptosis in a dose-dependent manner; at 1.2 μM, the total apoptosis rate reached approximately 40%, comparable to positive controls.
分子量

414.56

Formula

C23H35FN6

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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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:
Topo I/II-IN-3
目录号:
HY-183330
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