GSK5182 is a potent, orally bioavailable inverse agonist that selectively targets ERRγ (IC50 = 79 nM) without affecting ERRα or ERα nuclear receptors. Additionally, it stimulates ROS production in hepatocellular carcinoma cells.
Cat.No
DC43810
Name
GSK5182
Chemical Properties
CAS
877387-37-6
Formula
C27H31NO3
MW
417.54
Storage
0°C (short term), -20°C (long term), desiccated
References
[1]. Kim JH, et al. Estrogen-related receptor γ is upregulated in liver cancer and its inhibition suppresses livercancer cell proliferation via induction of p21 and p27. Exp Mol Med. 2016 Mar 4;48:e213.
[2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272.
[3]. Kim DK, et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes. 2013 Sep;62(9):3093-102.
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