1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Topoisomerase PI3K Apoptosis Reactive Oxygen Species
  3. Topoisomerase I/II inhibitor 3

Topoisomerase I/II inhibitor 3 

目录号: HY-146504
产品使用指南

Topoisomerase I/II inhibitor 3 (7) 是一种有效的拓扑异构酶 I (Topo I)II (Topo II) 双抑制剂。Topoisomerase I/II inhibitor 3 通过抑制 PI3K/Akt/mTOR 信号通路抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 可用于肝癌的研究。

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Topoisomerase I/II inhibitor 3 Chemical Structure

Topoisomerase I/II inhibitor 3 Chemical Structure

CAS No. : 2770804-74-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

PI3K

 

体外研究
(In Vitro)

Topoisomerase I/II inhibitor 3 (compound 7) (0-100 μM) can insert into DNA and change the topology of DNA, cause DNA damage to a certain extent[1].
Topoisomerase I/II inhibitor 3 (0-4 μM, 24 h) inhibits HCC (hepatocellular carcinoma) cells proliferation in a dose-dependent manner, inhibits migration and invasion of LM9 and HuH7 cells by inhibiting the expression of MMP-9[1].
Topoisomerase I/II inhibitor 3 (0-14 μM, 48 h) significantly induces the apoptosis of LM9 and HuH7 cells, and induces mitochondrial dysfunction and ROS burst in a dose-dependent manner[1].
Topoisomerase I/II inhibitor 3 (0-7 μM, 48 h) reduces the expression of the inhibitory factor Bcl-2 and promotes the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway[1].

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

Cell Proliferation Assay

Cell Line: HCC cells (HuH7 and LM9)[1]
Concentration: 0, 0.5, 1, 2, and 4 μM
Incubation Time: 24 h
Result: Inhibited HCC cells proliferation in a dose-dependent manner, with IC50 values of 2.10 μM (LM9) and 1.93 μM (HuH7), respectively, and dose-dependently inhibited the formation of cell colonies.

Apoptosis Analysis

Cell Line: LM9 and HuH7 cells[1]
Concentration: 0, 1.8, 3.5, 7, and 14 μM
Incubation Time: 48 h
Result: Significantly induced the apoptosis of LM9 and HuH7 cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: LM9 and HuH7 cells[1]
Concentration: 0, 1.8, 3.5, and 7 μM
Incubation Time: 48 h
Result: Reduced the expression of the inhibitory factor Bcl-2 and promoted the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibited the phosphorylation of PI3K/Akt/mTOR signaling pathway.
体内研究
(In Vivo)

Topoisomerase I/II inhibitor 3 (compound 7) (male Kunming mice, 0-400 mg/kg, IP, once) causes the mice in the 400 mg/kg group die, with the LD50 between 250 and 400 mg/kg[1].

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

Animal Model: Male Kunming mice (19-22 mg, 8 mice, 4 groups)[1]
Dosage: 200, 250, 400 mg/kg (dissolved in 5% DMSO and castor oil)
Administration: IP, once
Result: Did not cause the mice in the 250 mg/kg and 200 mg/kg groups die after 2 weeks of administration, and caused the mice in the 400 mg/kg group die, with the LD50 between 250 and 400 mg/kg.
分子量

404.46

Formula

C24H24N2O4

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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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 I/II inhibitor 3
目录号:
HY-146504
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