(E/Z)-GSK5182 是 (E)-GSK5182 和 (Z)-GSK5182 的消旋体。GSK5182 是一种高效选择性，具有口服活性的 ERRγ 反向激动剂，其 IC50 值为 79 nM。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。
货号:ajcx17224
CAS:N/A
分子式:C27H31NO3
分子量：417.54
溶解度:DMSO: 100 mg/mL (239.50 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM[1]. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma[1][2][3].

[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.