GSK5182
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).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.10%
- CAS. Nr.: 877387-37-6
- Formel: C27H31NO3
- Molecular Weight:417.55
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) GSK5182
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Biologische Aktivität
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ERRγ 79 nM (IC50) |
Reactive Oxygen Species |
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.
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Cell Line:The human hepatoma cell line PLC/PRF/5
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Concentration:0 μM, 10 μM, 20 μM
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Incubation Time:0 hour, 24 hours, 48 hours, 72 hours
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Result:Led to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.
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Cell Line:The human hepatoma cell line PLC/PRF/5
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Concentration:0 μM, 10 μM, 20 μM
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Incubation Time:24 hours
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Result:Caused a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of p-pRb.
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Cell Line:The human hepatoma cell line PLC/PRF/5
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Concentration:10 μM, 20 μM
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Incubation Time:
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Result:Induced cell cycle arrest.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice[3]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice
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Result:Inhibited the transcriptional activity of ERRγ, suppressed hepatic glucose production through inhibition of hepatic gluconeogenesis.
Chemical Information
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CAS. Nr. 877387-37-6
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Appearance Solid
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Molecular Weight 417.55
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Formel C27H31NO3
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Color White to off-white
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SMILES
OCCC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C3=CC=C(OCCN(C)C)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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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Journal Impact Factor
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Most Recent
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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
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (59.87 mM); Suspended solution; Need ultrasonic
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (419 KB)
- English - EN (419 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
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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