Fatostatin

Catalog No.S9785 Synonyms: 125B11

For research use only.

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.

Fatostatin Chemical Structure

CAS No. 125256-00-0

Selleck's Fatostatin has been cited by 3 Publications

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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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 294.41
Formula

C18H18N2S

CAS No. 125256-00-0
Storage 3 years -20°C powder
2 years -80°C in solvent

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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