GSK5182

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) [1][2][3].

Product Specifications

CAS Number

[877387-37-6]

UNSPSC

12352005

Hazard Statement

H360, H362

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

Applications

Cancer-programmed cell death

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/gsk5182.html

Purity

99.10

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

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

Molecular Formula

C27H31NO3

Molecular Weight

417.55

Precautions

H360, H362

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.