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Chetomin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Chetomin图片
CAS NO:1403-36-7
包装:1mg
市场价:3700元

产品介绍
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].

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].

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].

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

710.87

性状

Solid

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°C3 years
In solvent-80°C6 months
-20°C1 month