ERRγ Inhibitor

GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC₅₀ of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).

ERRγ-IN-1 is a ERRγ inhibitor with an IC₅₀ of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma.

2-Ethylhexyl diphenyl phosphate is an organophosphate flame retardants (OPFRs) and a PPARG agonist (EC₂₀: 2.04 µM). 2-Ethylhexyl diphenyl phosphate also inhibits ERRγ transcriptional activity (IC₅₀: 1.3 µM). 2-Ethylhexyl diphenyl phosphate upregulates 3β-HSD1, human chorionic gonadotropin (hCG) and progesterone secretion. 2-Ethylhexyl diphenyl phosphate can be used in studies of female reproduction and fetal development.