GSK5182

• 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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  ERRγ