2. Vitamin D Related/Nuclear Receptor NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Estrogen Receptor/ERR Reactive Oxygen Species
  4. GSK5182

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.

GSK5182 Chemical Structure

GSK5182 Chemical Structure

CAS No. : 877387-37-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 143 In-stock
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10 mM * 1 mL in DMSO USD 143 In-stock
Solid
1 mg USD 61 In-stock
5 mg USD 130 In-stock
10 mg USD 190 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of GSK5182:

GSK5182 Related Antibodies

Top Publications Citing Use of Products

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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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].

IC50 & Target[1][2]

ERRγ

79 nM (IC50)

Reactive Oxygen Species

 

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.

GSK5182 Related Antibodies

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.
Molecular Weight

417.55

Formula

C27H31NO3
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3949 mL 11.9746 mL 23.9492 mL
5 mM 0.4790 mL 2.3949 mL 4.7898 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.85%

COA (247 KB) HNMR (185 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK5182877387-37-6GSK 5182GSK-5182Estrogen Receptor/ERRReactive Oxygen SpeciesInhibitorinhibitorinhibit

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