1. Others
    Metabolic Enzyme/Protease
    Immunology/Inflammation
    NF-κB
  2. Estrogen Receptor/ERR
    Reactive Oxygen Species
  3. GSK5182

GSK5182 

Cat. No.: HY-111226
Handling Instructions

GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces Reactive Oxyen Species (ROS) generation in hepatocellular carcinoma (HCC).

For research use only. We do not sell to patients.

GSK5182 Chemical Structure

GSK5182 Chemical Structure

CAS No. : 877387-37-6

Size Stock
1 mg   Get quote  
5 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and 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].

IC50 & Target[2]

ERRγ

79 nM (IC50)

In Vitro

GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells[1].
GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb)[1].
GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase[1].

Cell Proliferation Assay[1]

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
Result: Led to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.

Western Blot Analysis[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 0 μM, 10 μM, 20 μM
Incubation Time: 24 hours
Result: Caused a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of p-pRb.

Cell Cycle Analysis[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 10 μM, 20 μM
Incubation Time:
Result: Induced cell cycle arrest.
In Vivo

GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production[3].

Animal Model: db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice[3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice
Result: Inhibited the transcriptional activity of ERRγ, suppressed hepatic glucose production through inhibition of hepatic gluconeogenesis.
Molecular Weight

417.54

Formula

C₂₇H₃₁NO₃

CAS No.

877387-37-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK5182
Cat. No.:
HY-111226
Quantity: