毛壳菌素|1403-36-7|-陌孚医药/Medlife

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毛壳菌素

目录号: PC10074 纯度: ≥98%

CAS No. :1403-36-7

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中文名称

毛壳菌素

中文别名

氨基磺酸镍;毛壳菌素

英文名称

英文别名

3,11a-Epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole-1,4-dione,2,3,5a,6,10b,11-hexahydro-3-(hydroxymethyl)-10b-[(1S,4S)-3-[[4-(hydroxymethyl)-5,7-dimethyl-6,8-dioxo-2,3-dithia-5,7-diazabicyclo[2.2.2]oct-1-yl]methyl]-1H-indol-1-yl]-2-methyl-,(3S,5aR,10bS,11aS)-;3,11a-Epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole-1,4-dione,2,3,5a,6,10b,11-hexahyd...;3,11a-Epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole-1,4-dione,2,3,5a,6,10b,11-hexahydro-3-(hydroxymethyl)-10b-[(1S,4;CHAETOMIN;Chetomin;CHETOMIN(RG);Chetomin,Chaetomin;Chetomin,Chaetomiumspecies;CS-1;CTM;NSC 289491;Stereoisomer of 2,3,5a,6,10b,11-hexahydro-3-(hydroxymethyl)-10b-[3-[[4-(hydroxymethyl)-5,7-dimethyl-6,8-dioxo-2,3-dithia-5,7-diazabicyclo[2.2.2]oct-1-yl]methyl]-1H-indol-1-yl]-2-methyl-3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole-1,4-dione;HSF4;SSFA2;DKFZp313O1039

Cas No.

1403-36-7

分子式

C₃₁H₃₀N₆O₆S₄

分子量

710.87

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

IC50 & Target[1][2]

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) .
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 HIF1αs N-terminus .

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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

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.
. Chetomin markedly decreases tumor formation in several murine models of NSCLC.

Medlife 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.

运输条件

Room temperature or refrigerated transportation.

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. [Information]

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