GSK-4716 Inhibitor

GSK4716 is an ERRbeta/gamma agonist (IC50 = 2uM) that can activate the receptor with similar potency as the protein ligand

1. Wang L, Zuercher W J, Consler T G, et al. X-ray Crystal Structures of the Estrogen-related Receptor- Ligand Binding Domain in Three Functional States Reveal the Molecular Basis of Small Molecule Regulation[J]. Journal of Biological Chemistry, 2006, 281 (49):37773-37781.
2. Wang SC, et al. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315 (1-2):146-52.
3. Rangwala S M, Wang X, Calvo J A, et al. Estrogen-related Receptor Is a Key Regulator of Muscle Mitochondrial Activity and Oxidative Capacity[J]. Journal of Biological Chemistry, 2010, 285 (29):22619-22629.

Small volumes of GSK-4716, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5751904 is an inhibitor targeting GSK-4716.