化合物 Topoisomerase I/II inhibitor 3 T61990

Product Introduction
Bioactivity


英文名: Topoisomerase I/II inhibitor 3

描述: Topoisomerase I/II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。 通过抑制 PI3K/Akt/mTOR 信号通路，Topoisomerase I/II inhibitor 3抑制细胞增殖、侵袭和迁移，诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 在肝癌中具有研究价值。

体外活性: 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 IC 50 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.

体内活性: 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 LD 50 between 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 LD 50 between 250 and 400 mg/kg.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途