SR-18292

For research use only.

Catalog No.S8528

2 publications

SR-18292 Chemical Structure

CAS No. 2095432-55-4

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

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

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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 ; 

PubMed: 28340340     


Co-IP of FLAG-PGC-1α following treatment with SR-18292 (10μM). IP, immunoprecipitation.

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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.18 mM)
Ethanol 73 mg/mL (199.18 mM)
Water Insoluble

* 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 366.50
Formula

C23 H30 N2 O2

CAS No. 2095432-55-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)CN(CC(COC2=CC=CC3=C2C=CN3)O)C(C)(C)C

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID