ERRγ-IN-1

ERRγ-IN-1 (Compound 18a) is a highly potent inverse agonist of ERRγ, with an IC₅₀ of 0.040 μM for binding to ERRγ. It shows extremely weak cross-reactivity with ERRα (IC₅₀ > 10 μM), moderate activity against ERRβ (IC₅₀ = 1.33 μM), and weak binding ability to ERα (IC₅₀ = 1.24 μM), indicating its targeting selectivity for ERRγ^[1].
ERRγ-IN-1 (6-12 μM) reduces the ERRγ mRNA expression level by approximately 90% and increases the NIS mRNA expression level by about 2-fold in CAL-62 anaplastic thyroid cancer cells, and this effect depends on the activation of MAPK (p44/p42)^[1].
ERRγ-IN-1 (6-12 μM) reduces ERRγ protein levels in a dose-dependent manner and promotes membrane localization of fully glycosylated NIS (the 98 kDa isoform) in CAL-62 ATC cells, a process dependent on the activation of MAPK (p44/p42)^[1].
ERRγ-IN-1 (6-12 μM) increases iodine uptake in CAL-62 anaplastic thyroid cancer cells by approximately 2-fold at 12 μM and 1.5-fold at 6 μM (measured as CPM/μg protein), and this effect depends on the activation of MAPK (p44/p42)^[1].
Combination of ERRγ-IN-1 and ¹³¹I reduces the colony-forming ability of CAL-62 cells by approximately 40%^[1].
ERRγ-IN-1 (10 μM) moderately inhibits CYP2D6 (63.5% of the control group) and CYP3A4 (66.4% of the control group), while exerts weak inhibitory effects on CYP1A2 (88% of the control group), CYP2C9 (86.1% of the control group) and CYP2C19 (81.2% of the control group)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.