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CAS No. : 1403-36-7
MCE 国际站:Chetomin
产品活性:Chetomin 作为 Chaetomium globosum 的活性成分,是一种热休克蛋白90/缺氧诱导因子1α (Hsp90/HIF1α) 途径的抑制剂。Chetomin 是一种有效的、无毒的非小细胞肺癌干细胞 (NSCLC CSC) 靶向分子。
研究领域:Cell Cycle/DNA Damage | Metabolic Enzyme/Protease | Apoptosis
作用靶点:HSP | Apoptosis
In Vitro: Chetomin (0~10 μM; 24 hours; H460 and H1299 cells) shows progressively lower expression of several survival-promoting proteins promoted by Hsp90/HIF1α activity, including insulin-like growth factor 1 (IGF1 R), epidermal growth factor receptor (EGFR), Src, mitogen-activated protein kinase kinase 1/2 (MEK1/2), activation of protein kinase B (Akt), and mammalian target of rapamycin (mTOR) .
Chetomin (0~10 μM; 24 hours; H1299 cells) elicits cell cycle arrest in susceptible and chemoresistant NSCLC cell lines.
. Chetomin (1 μM; 3 days; H460 and H1299 cells) pretreatment abolishes their sphere-forming capacity. Chetomin inhibits sphere-forming by NSCLC CSCs within a nanomolar range, and proliferation of susceptible and chemoresistant NSCLC non-CSCs within a micromolar range. Chetomin (24 h) decreases HIF-response element activity in H460 and H1299 monolayer cultures. Chetomin (0~10 μM) specifically inhibits the Hsp90-HIF1α binding interaction in HIF1α's N-terminus .
In Vivo: Chetomin (0~100 mg/kg; p.o.) inhibits lung tumorigenesis in NSCLC mouse models.
Chetomin markedly decreases tumor formation in several murine models of NSCLC.
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