GSK5182
Product Specifications
UNSPSC Description
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].
Target Antigen
Estrogen Receptor/ERR; Reactive Oxygen Species
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
99.85
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 Weight
417.55
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-111226/GSK5182-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-111226/GSK5182-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
877387-37-6
Available Sizes
Curated Selection
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