SR-18292

Catalog No.S8528

For research use only.

SR-18292 inhibits PGC-1α gluconeogenic activity and reduces co-activation of HNF4α by modulating the interaction between GCN5 and PGC-1α.

SR-18292 Chemical Structure

CAS No. 2095432-55-4

Selleck's SR-18292 has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description SR-18292 inhibits PGC-1α gluconeogenic activity and reduces co-activation of HNF4α by modulating the interaction between GCN5 and PGC-1α.
Targets
PGC-1α [1]
In vitro

SR-18292 is a potent inhibitor of the gluconeogenic gene expression and glucose production in hepatocytes. It increases the interaction of PGC-1α with GCN5 and reduces co-activation of HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function[2].

Assay
Methods Test Index PMID
Western blot PGC1-α / GCN5 28340340
In vivo SR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity and improves glucose homeostasis in dietary and genetic mouse models of type 2 diabetes. SR-18292 suppresses hepatic glucose production and increases liver insulin sensitivity in vivo. The liver is a major target of SR-18292 and probably accounts for a significant part of its anti-diabetic effects[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: U-2 OS cells overexpressing Ad-GCN5
  • Concentrations: 10 μM
  • Incubation Time: 18 h
  • Method:

    For determination of GCN5 HAT activity U-2 OS cells overexpressing Ad-GCN5 are treated with SR-18292 (10μM) for 18 h. Cells are lysed with buffer B (20 mM HEPES-KOH (pH 7.9), 125 mM NaCl, 1 mM EDTA, 1 mM DTT, 1% IGEPAL (v/v), 10% glycerol (v/v), 5 mM NaF, 5 mM β-glycerophosphate, 5 mM sodium butyrate and 10 mM nicotinamide), supplemented with Protease Inhibitor Cocktail. FLAG-GCN5 is immunoprecipitated with FLAG beads overnight at 4℃ following multiple washes with lysis buffer. GCN5 is then eluted using 3× FLAG peptide and the purified protein is used to determine HAT activity using the HAT Inhibitor Screening Assay Kit.

Animal Research:

[1]

  • Animal Models: a high fat diet (HFD) fed mice, a dietary model of obesity and type 2 diabates
  • Dosages: 45 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 366.50
Formula

C23 H30 N2 O2

CAS No. 2095432-55-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(C=C1)CN(CC(COC2=CC=CC3=C2C=CN3)O)C(C)(C)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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