1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. Chetomin

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.

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Chetomin Chemical Structure

Chetomin Chemical Structure

CAS No. : 1403-36-7

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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[1].

IC50 & Target[1]

HSP90

 

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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

710.87

Formula

C31H30N6O6S4

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N2[C@]3([H])[C@](C4=CC=CC=C4N3)(N5C6=CC=CC=C6C(C[C@@]7(N8C)C(N([C@](SS7)(CO)C8=O)C)=O)=C5)C[C@]29C(N(C)[C@]1(SS9)CO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥99.0%

References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Chetomin
Cat. No.:
HY-107553
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