GSK5182

GSK5182 is a selective, orally active small-molecule inverse agonist of the orphan nuclear receptor estrogen-related receptor gamma (ERRγ, encoded by ESRRG) with an IC50 of approximately 77–79 nM. Developed originally by GlaxoSmithKline as a tamoxifen analog, GSK5182 exhibits high selectivity for ERRγ over other nuclear receptors, including ERRα, ERRβ, and estrogen receptor alpha (ERα). As a chemical tool, GSK5182 has been widely investigated in preclinical research for its therapeutic potential in various metabolic, inflammatory, and oncological conditions. It has been shown to suppress hepatic gluconeogenesis in type 2 diabetes models, prevent vascular calcification by downregulating BMP2 signaling, ameliorate cartilage degeneration in osteoarthritis models, inhibit osteoclastogenesis, and enhance sodium/iodide symporter (NIS) expression and radioiodine uptake in anaplastic thyroid cancer cells.

Other names

(E/Z)-GSK5182(Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol4-hydroxytamoxifen analog