Topoisomerase I/II inhibitor 3 (7) 是一种有效的拓扑异构酶 I (Topo I)和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。
| 生物活性 | TopoisomeraseI/II inhibitor 3 (compound 7) is a potenttopoisomeraseI (Topo I)andII (Topo II)dual inhibitor.TopoisomeraseI/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induceapoptosisby inhibitingPI3K/Akt/mTOR signaling pathway.TopoisomeraseI/II inhibitor 3 can be used for livercancerresearch[1]. |
| IC50& Target | Topoisomerase I | Topoisomerase II | PI3K |
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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].
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 IC50values 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. |
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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 LD50between 250 and 400 mg/kg[1].
| 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 LD50between 250 and 400 mg/kg. |
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| 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. |
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