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。
| 生物活性 | Chetomin, an active component of Chaetomium globosum, is aheat shock protein90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancercancer stem cells(NSCLC CSC)-targeting molecule[1]. |
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体外研究
(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)[1].
Chetomin (0~10 μM; 24 hours; H1299 cells) elicits cell cycle arrest in susceptible and chemoresistant NSCLC cell lines[1].
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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[1].
Western Blot Analysis[1] | Cell Line: | H460 and H1299 cells | | Concentration: | 0~10 μM | | Incubation Time: | 24 hours | | Result: | Showed 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). |
Cell Cycle Analysis[1] | Cell Line: | H1299 cells | | Concentration: | 0~10 μM | | Incubation Time: | 24 hours | | Result: | Elicited cell cycle arrest in susceptible and chemoresistant NSCLC cell lines. |
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体内研究
(In Vivo) | Chetomin (0~100 mg/kg; p.o.) inhibits lung tumorigenesis in NSCLC mouse models[1].
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Chetomin markedly decreases tumor formation in several murine models of NSCLC[1].
| Animal Model: | Mouse | | Dosage: | 0~100 mg/kg | | Administration: | P.o. | | Result: | Inhibited lung tumorigenesis in NSCLC mouse models. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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