(E/Z) -GSK5182

(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].

Product Specifications

CAS Number

[2699724-40-6]

UNSPSC

12352005

Target

Estrogen Receptor/ERR; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB; Vitamin D Related/Nuclear Receptor

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/e-z-gsk5182.html

Purity

98.90

Solubility

DMSO : ≥ 75 mg/mL

Smiles

OCCC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCN(C)C)\C3=CC=C(C=C3)O

Molecular Formula

C27H31NO3

Molecular Weight

417.54

References & Citations

[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.