Topoisomerase I/II inhibitor 2

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Topoisomerase I/II inhibitor 2 

Topoisomerase I/II inhibitor 2 (compound 1a) 是一种有效的拓扑异构酶 (Topoisomerase) 抑制剂,Huh7 与 LM9 细胞中的 IC50 分别为 9.82 μM 和 6.83 μM。Topoisomerase I/II inhibitor 2 对 DNA 拓扑异构酶 I/II 具有双重抑制,也能抑制小鼠模型中的异种移植肿瘤。Topoisomerase I/II inhibitor 2 具有治疗肝癌的潜在价值。

Topoisomerase I/II inhibitor 2

Topoisomerase I/II inhibitor 2 Chemical Structure

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生物活性

Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in treating liver cancer[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

体外研究
(In Vitro)

Topoisomerase I/II inhibitor 2 (compound 1a) (0-150 μM; 72 hours) has favourable anti-proliferative activity in cancer cell lines, and better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9)[1].
Topoisomerase I/II inhibitor 2 (20 μM; 24 hours) has no damage to the DNA of HuH7 cells while some damage is noticed on LM9 cells[1].
Topoisomerase I/II inhibitor 2 (1.25-8 μM; 1-2 weeks) inhibits cell proliferation of LM9 and Huh7 in a concentration-dependent manner[1].
Topoisomerase I/II inhibitor 2 (1.25-8 μM; 24 hours) has a good inhibitory effect on the migration and invasion of LM9 and HuH7 cells with concentration-dependent manner[1].
Topoisomerase I/II inhibitor 2 (0-20 μM; 24 hours) can inhibit the expression of matrix metalloproteinases-9 (MMP-9) in LM9 and HuH7 cells[1].
Topoisomerase I/II inhibitor 2 (0-20 μM; 48 hours) inhibits cells proliferation by blocking cell cycle at the G2/M phase[1].
Topoisomerase I/II inhibitor 2 (3.5-20 μM; 48 hours) can injure mitochondrial function and induce cell apoptosis in a concentration-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: LM9, HuH7, SK-hep-1, HepG2, HT-29, HCT-116, RKO, SW480, MCF-7, MDA-B-231, HGC-27, SGC-7901, BGC-823, A549, U251, HL-60, LO2[1]
Concentration: 0-150 μM
Incubation Time: 72 hours
Result: Displayed favourable anti-proliferative activity and had better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9).

Western Blot Analysis

Cell Line: LM9 and HuH7 cells[1]
Concentration: 0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7
Incubation Time: 48 hours
Result: Inhibited the expression of MMP-9.

Cell Cycle Analysis

Cell Line: LM9 and HuH7 cells[1]
Concentration: 0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7
Incubation Time: 48 hours
Result: Inhibited cells proliferation by blocking cell cycle at the G2/M phase.

Apoptosis Analysis

Cell Line: LM9 and HuH7 cells[1]
Concentration: 3.5, 7, 14 μM in LM9; 5, 10, 20 μM in HuH7
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner.

分子量

336.34

Formula

C19H16N2O4

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.

参考文献
  • [1]. Deng X, et al. Design, synthesis and anti-hepatocellular carcinoma activity of 3-arylisoquinoline alkaloids. Eur J Med Chem. 2022;228:113985.

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