| Name | GSK-4716 |
| Description | GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand |
| 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[3] |
| In vitro | GSK4716 was a selective ERRbeta/gamma agonist[1].?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[2].GSK4716 has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise[3] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (14.17 mM), Sonication is recommended.
DMSO : 100 mg/mL (354.18 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | GSK-4716 | GSK4716 | GSK 4716 | EstrogenReceptor | Estrogen Receptor/ERR | Estrogen Receptor | ERRβ/γ | ERR |
| Inhibitors Related | Tamoxifen | Estradiol | 2-Ethylhexyl trans-4-methoxycinnamate | Diisopropyl phthalate | Estradiol benzoate | Bisphenol B | Mequinol | Phthalic acid | Chlorothalonil | Ethisterone | Tamoxifen Citrate | Cholesterol |
| Related Compound Libraries | Nuclear Receptor Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Ovarian Cancer Compound Library | NO PAINS Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
