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CAS No. : 2768599-97-7
MCE 国际站:GLS1 Inhibitor-4
产品活性:GLS1 Inhibitor-4 (compound 41e) 是一种有效的 GLS1 抑制剂,IC50 为 11.86 nM。GLS1 Inhibitor-4 显示出抗增殖活性、良好的代谢稳定性和强大的 GLS1 结合亲和力。GLS1 Inhibitor-4 阻断谷氨酰胺代谢并诱导 ROS 的产生。GLS1 Inhibitor-4 可诱导细胞凋亡 (apoptosis)并显示出抗肿瘤活性。
研究领域:Metabolic Enzyme/Protease | Apoptosis
作用靶点:Glutaminase | Apoptosis
In Vitro: GLS1 Inhibitor-4 (compound 41e) shows antiproliferative activity with IC50s of 0.051, 0.37, 0.32, 1.34 µM for HCT116 and MDA-MB-436, CT26, H22 cells, respectively.
GLS1 Inhibitor-4 shows good plasma and liver microsomal stability with 96% stability in Human plasma.
GLS1 Inhibitor-4 shows robust binding affinity with GLS1 protein, the dissociation constants (Kd) of 52 nM.
GLS1 Inhibitor-4 (0.1, 0.5, 1 µM) inhibits the colony formation of HCT116 cells in a dose-dependent manner.
GLS1 Inhibitor-4 (100, 300 nM, 12 h) reduces the concentration of a number of key metabolites downstream of glutamate within 12 h.
GLS1 Inhibitor-4 (30, 50, 200 nM; 6 h) increases the ROS levels in a dose-dependent manner in HCT116 cells.
GLS1 Inhibitor-4 (1 mmol/L; 12 h) significantly decreases the ATP production basal and maximal OCRs (oxygen consumption rates) after 12 h, suppresses the aerobic glycolysis in HCT116 cancer cells.
GLS1 Inhibitor-4 (30, 50, 200 nM; 24 h) induces apoptosis in a dose-dependent manner.
In Vivo: GLS1 Inhibitor-4 (50, 100 mg/kg; i.p.; twice a day for 21 consecutive days) shows antitumor activity in a dose-dependent manne.
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