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MedChemExpress - Model Chetomin - ...

MedChemExpress - Model Chetomin - 1403-36-7

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].

Chetomin

MCE China：Chetomin

Brand：MedChemExpress (MCE)

Cat. No.HY-107553

CAS：1403-36-7

Purity：95.3%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

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].

IC50 & Target：HSP90

References：

[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. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。