Chetomin

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Chetomin  纯度: ≥99.0%

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。

Chetomin

Chetomin Chemical Structure

CAS No. : 1403-36-7

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生物活性

Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule[1].

IC50 & Target[1]

HSP90

 

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].
. 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

Chetomin (0~100 mg/kg; p.o.) inhibits lung tumorigenesis in NSCLC mouse models[1].
. Chetomin markedly decreases tumor formation in several murine models of NSCLC[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse
Dosage: 0~100 mg/kg
Administration: P.o.
Result: Inhibited lung tumorigenesis in NSCLC mouse models.

分子量

710.87

Formula

C31H30N6O6S4
CAS 号

1403-36-7
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
参考文献

  • [1]. Min S, et al. Chetomin, a Hsp90/HIF1α pathway inhibitor, effectively targets lung cancer stem cells and non-stem cells. Cancer Biol Ther. 2020;21(8):698-708.

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