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GSK5182

Catalog No. T8370   CAS 877387-37-6

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

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GSK5182 Chemical Structure
GSK5182, CAS 877387-37-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 68.00
5 mg In stock $ 97.00
10 mg In stock $ 155.00
25 mg In stock $ 289.00
50 mg In stock $ 438.00
100 mg In stock $ 647.00
1 mL * 10 mM (in DMSO) In stock $ 116.00
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Purity: 97.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)
Targets&IC50 ERRγ:79 nM (IC50)
In vitro Small interfering RNA (siRNA)-mediated knockdown of ERRγ (siRNA-ERRγ) or an ERRγ inverse agonist, GSK5182, were also used to examine the effects of ERRγ inhibition on the proliferation and growth of a human hepatoma cell line, PLC/PRF/5[1].
In vivo a hyperinsulinemic-euglycemic clamp study and long-term studies of the antidiabetic effects of GSK5182, the ERRγ-specific inverse agonist, in db/db and DIO mice demonstrated that GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production[2].
Cell Research Cell Line:The human hepatoma cell line PLC/PRF/5. Concentration:0 μM, 10 μM, 20 μM. Incubation Time:0 hour, 24 hours, 48 hours, 72 hours
Molecular Weight 417.54
Formula C27H31NO3
CAS No. 877387-37-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/ml (143.7 mM)

TargetMolReferences and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries:
NF-κB Signaling Compound Library Oxidation-Reduction Compound Library Anti-Breast Cancer Compound Library Anti-Ovarian Cancer Compound Library NO PAINS Compound Library Pyroptosis Compound Library Mitochondria-Targeted Compound Library Immunology/Inflammation Compound Library Metabolism Compound Library Bioactive Compound Library

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Keywords

GSK5182 877387-37-6 Endocrinology/Hormones Immunology/Inflammation Metabolism NF-Κb Reactive Oxygen Species Estrogen/progestogen Receptor Estrogen Receptor/ERR GSK-5182 inhibit GSK 5182 Inhibitor inhibitor

 

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