SR-18292

Catalog No.S8528 Batch:S852802

Technical Data

Formula

C₂₃ H₃₀ N₂O₂

Molecular Weight

366.50

CAS No.

2095432-55-4

Solubility (25°C)*

In vitro

DMSO

73 mg/mL (199.18 mM)

Ethanol

73 mg/mL (199.18 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

5.1mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 102 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].

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 Assay:^{^[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 Study:^{^[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.

Cell Assay:^{^[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 Study:^{^[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.

References

[1] Sharabi K, et al. Cell. 2017, 169(1):148-160.

Selleck's SR-18292 has been cited by 6 publications

Small molecules targeting selective PCK1 and PGC-1α lysine acetylation cause anti-diabetic action through increased lactate oxidation [ Cell Chem Biol, 2024, 31(10):1772-1786.e5]	PubMed: 39341205
Mocetinostat activates Krüppel-like factor 4 and protects against tissue destruction and inflammation in osteoarthritis [ JCI Insight, 2023, 8(17)e170513]	PubMed: 37681413
Mocetinostat activates Krüppel-like factor 4 and protects against tissue destruction and inflammation in osteoarthritis [ JCI Insight, 2023, 8(17)e170513]	PubMed: 37681413
Propionate promotes gluconeogenesis by regulating mechanistic target of rapamycin (mTOR) pathway in calf hepatocytes [ Anim Nutr, 2023, 10.1016/j.aninu.2023.07.001]	PubMed: 37841648
Kaempferol Alleviates Oxidative Stress and Apoptosis Through Mitochondria-dependent Pathway During Lung Ischemia-Reperfusion Injury [ Front Pharmacol, 2021, 12:624402]	PubMed: 33746757
Combined Targeting of Estrogen Receptor Alpha and Exportin 1 in Metastatic Breast Cancers [ Cancers (Basel), 2020, 12(9)E2397]	PubMed: 32847042

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.