Fatostatin

For research use only.

Catalog No.S9785 Synonyms: 125B11

1 publication

Fatostatin Chemical Structure

CAS No. 125256-00-0

Fatostatin (125B11), a diarylthiazole derivative, is a specific inhibitor of Sterol regulatory element binding proteins (SREBPs) activation. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin suppresses growth and enhances apoptosis in cancer cells.

Selleck's Fatostatin has been cited by 1 publication

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Biological Activity

Description

Fatostatin (125B11), a diarylthiazole derivative, is a specific inhibitor of Sterol regulatory element binding proteins (SREBPs) activation. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin suppresses growth and enhances apoptosis in cancer cells.

Targets
SREBP [1]
()
In vitro

Fatostatin impairs the activation process of sterol regulatory element binding proteins (SREBPs), thereby decreasing the transcription of lipogenic genes in cells. Fatostatin inhibits the ER-Golgi translocation of SREBPs through binding to their escort protein, the SREBP cleavage-activating protein (SCAP), at a distinct site from the sterol-binding domain.[1]

In vivo

Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. Fatostatin may serve as a tool for gaining further insights into the regulation of SREBP.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: CHO-K1 cells
  • Concentrations: 20 μM
  • Incubation Time: 20 h
  • Method:

    CHO-K1 cells are plated out onto a 96-well plate in medium A. The cells are transiently cotransfected with pCMV-PLAP-BP2, pCMV-SCAP, and pAc-b-gal, using Lipofectamine reagent. After incubation for 5 hr, the cells are washed with PBS and then incubated in medium B, in the absence or presence of fatostatin (20 μM) or sterols (10 μg/mL cholesterol and 1 μg/mL 25-hydroxycholesterol). After 20 hr of incubation, an aliquot of the medium is assayed for secreted alkaline phosphatase activity. The cells in each well are lysed and used for measurement of b-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of b-galactosidase.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 4-to-5-week-old homozygous male obese (ob/ob) mice (C57BL/6J)
  • Dosages: 30 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (254.74 mM)
Water Insoluble
Ethanol '''''75 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 294.41
Formula

C18H18N2S

CAS No. 125256-00-0
Storage powder
in solvent
Synonyms 125B11

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID