Cat. No.: HY-111226

GSK5182

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

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).

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

Purity: 99.10%
CAS No.: 877387-37-6
Formula: C₂₇H₃₁NO₃
Molecular Weight:417.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK5182 Chemical Structure

CAS No.: 877387-37-6

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]

ERRγ

79 nM (IC₅₀)

Reactive Oxygen Species

All Estrogen Receptor/ERR Isoforms :

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 877387-37-6
Appearance Solid
Molecular Weight 417.55
Formula C₂₇H₃₁NO₃
Color White to off-white
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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Environ Sci Technol

Binding and Activation of Estrogen-Related Receptor γ: A Novel Molecular Mechanism for the Estrogenic Disruption Effects of DDT and Its Metabolites. [Abstract]

2022 Sep 6;56(17):12358-12367. PMID: 35947429
J Hazard Mater

Estrogenic and transgenerational effects of perfluorocarboxylic acids through estrogen-related receptor γ pathway. [Abstract]

2025 Sep 5:495:138994. PMID: 40555023
Oncol Res

ERRγ Promotes Multiple Myeloma Survival by Coordinating NF-κB Signaling and Mitochondrial Apoptosis Regulation. [Abstract]

2025 Aug 28;33(9):2399-2420. PMID: 40918468
Sci Total Environ

Activation of estrogen-related receptor: An alternative mechanism of hexafluoropropylene oxide homologs estrogenic effects. [Abstract]

2023 Nov 25:901:166257. PMID: 37574057

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (59.87 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3949 mL

11.9746 mL

23.9492 mL

5 mM

0.4790 mL

2.3949 mL

4.7898 mL

10 mM

0.2395 mL

1.1975 mL

2.3949 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 25 mg/mL (59.87 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

[2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3949 mL	11.9746 mL	23.9492 mL	59.8731 mL
	5 mM	0.4790 mL	2.3949 mL	4.7898 mL	11.9746 mL
	10 mM	0.2395 mL	1.1975 mL	2.3949 mL	5.9873 mL
	15 mM	0.1597 mL	0.7983 mL	1.5966 mL	3.9915 mL
	20 mM	0.1197 mL	0.5987 mL	1.1975 mL	2.9937 mL
	25 mM	0.0958 mL	0.4790 mL	0.9580 mL	2.3949 mL
	30 mM	0.0798 mL	0.3992 mL	0.7983 mL	1.9958 mL
	40 mM	0.0599 mL	0.2994 mL	0.5987 mL	1.4968 mL
	50 mM	0.0479 mL	0.2395 mL	0.4790 mL	1.1975 mL

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GSK5182

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK5182

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK5182

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK5182

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK5182 Related Classifications

HY-111226 Related Classifications