GSK-4716

SKU: orb1301719

Description

GSK4716 is a small molecule agonist of the ERRβ and ERRγ receptors with an IC50 of 2 μM, demonstrating potency comparable to endogenous protein ligands. This compound is a valuable research tool for investigating ERR-mediated transcriptional regulation in metabolic, neurodegenerative, and cancer-related studies using both cellular and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 101574-65-6
• MW: 282.34
• Purity: 99.53%
• Formula: C₁₇H₁₈N₂O₂
• SMILES: CC(C)c1ccc(\C=N\NC(=O)c2ccc(O)cc2)cc1
• Target: Estrogen Receptor/ERR
• Solubility: DMSO:100 mg/mL (354.18 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (14.17 mM)

Bioactivity

• In Vitro:
  GSK4716 was a selective ERRbeta/gamma agonist. ERRbeta is transiently induced, and ERRgamma is dramatically induced (and accumulates) in a differentiation-dependent manner in skeletal muscle cells. Treatment of differentiated skeletal muscle cells with the ERRbeta/gamma agonist (GSK4716) produced a significant increase in the expression of GRalpha (isoform D) .the mRNAs encoding the glucocorticoid receptor (GR), 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1), the enzyme that converts inactive cortisone to cortisol and hexose-6-phosphate dehydrogenase expression (H6PDH) that stimulates oxoreduction by 11beta-HSD1.the mRNAs encoding characterized GR target genes, including C/EBP, ApoD and Monoamine oxidase-A (MAO-A) are induced in GSK4716 treated cells.GSK4716 has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise
• Cell Research:
  Mouse myoblasts were isolated as described previously. Human ERRγ-IRES green fluorescent protein adenovirus was generated by Welgen. Following a 48-h differentiation period, myotubes were transduced with green fluorescent protein or ERRγ adenovirus for 48 h. The titers to achieve low and high levels of ERRγ expression were 1* 10^8 and 5*10^8 virus particles/ml, respectively. GSK4716 was synthesized as described previously and dissolved in DMSO for cell culture experiments. Cells treated with a corresponding volume of DMSO were used as controls

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, GSK 4716, GSK4716, GSK-4716, Estrogen Receptor/ERR, EstrogenReceptor, Estrogen Receptor, ERR, ERRβ/γ

Compound Identifiers

PubChem CID

5331325