GSK0660
Based on 15 publication(s) in Google Scholar
GSK0660 is a potent PPARβ antagonist with an IC50 of 155 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.49%
- No. CAS: 1014691-61-2
- Fòrmula: C19H18N2O5S2
- Peso molecular:418.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK0660
More- J Adv Res. 2020 Jun 20;27:115-125. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Cell Death Discov. 2024 Jul 19;10(1):329. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Cell Mol Life Sci. 2025 Oct 30;82(1):375. [Abstract]
- Biochem Pharmacol. 2025 Jun 9:117039. [Abstract]
- Food Funct. 2024 May 20;15(10):5485-5495. [Abstract]
- Liver Int. 2023 Dec;43(12):2808-2823. [Abstract]
- Eur J Pharmacol. 2026 Jul 10:1029:179008. [Abstract]
- FASEB J. 2024 Dec 15;38(23):e70212. [Abstract]
- Chem Res Toxicol. 2024 Sep 16;37(9):1574-1587. [Abstract]
- Brain Res Bull. 2018 Jun:140:378-391. [Abstract]
- PPAR Res. 2020 Dec 22:2020:8864813. [Abstract]
- J Cell Biochem. 2024 Dec 4:e30685. [Abstract]
- Microvasc Res. 2023 Jul:148:104531. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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WB
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Flow Cytometry
Actividad biológica
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PPARβ/δ 155 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C2C12 | IC50 |
48 nM
Compound: GSK0660
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Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis
Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis
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[PMID: 22369181] |
GSK0660 is a potent antagonist of PPARβ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both >10 μM. GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.8. GSK0660 (100 nM) reduces CPT1a (a PPARβ/δ target gene) expression below the basal vehicle-treated level by approximately 50%, but shows no effect on PDK4 expression, which is also a PPARβ/δ target gene in skeletal muscle cells[1].
GSK0660 (0.5 μM) reduces the levels of AMPK and eNOS phosphorylation, and BMP-2, Runx-2 mRNA expression in MC3T3-E1 cells. GSK0660 (0.1 and 0.5 μM) reverses the bezafibrate-induced enchancement of ALP activity on d 7 in MC3T3-E1 cells[2].
GSK0660 (1 μM) markedly blocks GW501516-mediated attenuation of glutamate release, and the effect of GW501516 on ROS generation in BV-2 cells stimulated with LPS. Furthermore, GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1014691-61-2
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Appearance Solid
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Peso molecular 418.49
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Fòrmula C19H18N2O5S2
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Color Light yellow to yellow
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SMILES
O=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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J Adv Res
2020 Jun 20;27:115-125. PMID: 33318871 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Cell Death Discov
2024 Jul 19;10(1):329. PMID: 39030174 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Cell Mol Life Sci
GLP-1 receptor agonist protects glucose-stimulated insulin secretion in pancreatic β-cells against lipotoxicity via PPARδ/UCP2 pathway. [Abstract]2025 Oct 30;82(1):375. PMID: 41165809 -
Biochem Pharmacol
ZLY032 mediated activation of Notch1/Hes1 signaling inhibits cardiomyocyte ferroptosis to protect against myocardial Ischemia-Reperfusion injury in mice. [Abstract]2025 Jun 9:117039. PMID: 40499841 -
Food Funct
Ginsenoside Rk1 improves endothelial function in diabetes through activating peroxisome proliferator-activated receptors. [Abstract]2024 May 20;15(10):5485-5495. PMID: 38690748 -
Liver Int
2023 Dec;43(12):2808-2823. PMID: 37833850 -
Eur J Pharmacol
DTMB attenuates hepatic inflammation and lipid dysregulation via PPAR-γ modulation in diet-induced steatohepatitis. [Abstract]2026 Jul 10:1029:179008. PMID: 42173393 -
FASEB J
Transcriptional and functional regulation of cell cycle and UV response by PPARβ in human skin epidermal cells. [Abstract]2024 Dec 15;38(23):e70212. PMID: 39620966
GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212. [Abstract]
Cell proliferation quantified using EdU uptake (left) and FACS analysis of the cell cycle progression (right) in control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) malignant human keratinocytes (SCC13).
GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212. [Abstract]
Expression of p21 at mRNA (CDKA1A, quantified by qPCR; left) and protein (representative western blot, middle panel; right panel represents the quantification of three independent western blots) in control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) SCC13 cells.
GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212. [Abstract]
Representative western blots (left) of three independent western blots (right) of phosphorylated H2AX (γH2AX) (upper panel), of total and phosphorylated CHK1 (middle panels), and of p21 at 0, 0.5, 2, and 6 h after UVB‐exposure in control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) SCC13 cells.
GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212. [Abstract]
Percentage of apoptotic cells in response to UVB exposure using FACS analysis of Annexin V on control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) SCC13 cells.
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Chem Res Toxicol
Novel Dual PPAR δ/γ Partial Agonist Induces Hepatic Lipid Accumulation through Direct Binding and Inhibition of AKT1 Phosphorylation, Mediating CD36 Upregulation. [Abstract]2024 Sep 16;37(9):1574-1587. PMID: 39235066 -
Brain Res Bull
Treatment with corn oil improves neurogenesis and cognitive performance in the Ts65Dn mouse model of Down syndrome. [Abstract]2018 Jun:140:378-391. PMID: 29935232 -
PPAR Res
Ligand-Activated Peroxisome Proliferator-Activated Receptor β/ δ Facilitates Cell Proliferation in Human Cholesteatoma Keratinocytes. [Abstract]2020 Dec 22:2020:8864813. PMID: 33424958 -
J Cell Biochem
2024 Dec 4:e30685. PMID: 39632616 -
Microvasc Res
Gastrodin protects endothelial cells against high glucose-induced injury through up-regulation of PPARβ and alleviation of nitrative stress. [Abstract]2023 Jul:148:104531. PMID: 36963481
Solvente y solubilidad
DMSO : ≥ 49 mg/mL (117.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell viability is determined by the MTT dye. MC3T3-E1 cells are incubated with bezafibrate (1−1000 μM) for 24, 48, or 72 h, and are pretreated with the AMPK inhibitor compound C (5 μM), PPARβ inhibitor GSK0660 (0.5 μM), PPARα inhibitor MK886 (10 μM), or NOS inhibitor L-NAME (1000 μM) followed by bezafibrate (100 μM) incubation for 48 h. After the incubations, 10 μL of MTT is added to each well of a 96-well microplate, and the microplates are placed in an incubator at 37°C for 4 h. One hundred fifty microliters of DMSO is added to all wells and mixed thoroughly to lyse the cells and dissolve the dark blue crystals. After 10 min, the absorbance is measured at 570 nm using a microplate reader[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Shearer BG, et al. Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist. Mol Endocrinol. 2008 Feb;22(2):523-9. Epub 2007 Nov 1. [Content Brief]
[2]. Zhong X, et al. Bezafibrate enhances proliferation and differentiation of osteoblastic MC3T3-E1 cells via AMPK and eNOS activation. Acta Pharmacol Sin. 2011 May;32(5):591-600. [Content Brief]
[3]. Lee WJ, et al. Activation of PPARδ attenuates neurotoxicity by inhibiting lipopolysaccharide-triggered glutamate release in BV-2 microglial cells. J Cell Biochem. 2018 Feb 1. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3895 mL | 11.9477 mL | 23.8954 mL | 59.7386 mL |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.7791 mL | 11.9477 mL | |
| 10 mM | 0.2390 mL | 1.1948 mL | 2.3895 mL | 5.9739 mL | |
| 15 mM | 0.1593 mL | 0.7965 mL | 1.5930 mL | 3.9826 mL | |
| 20 mM | 0.1195 mL | 0.5974 mL | 1.1948 mL | 2.9869 mL | |
| 25 mM | 0.0956 mL | 0.4779 mL | 0.9558 mL | 2.3895 mL | |
| 30 mM | 0.0797 mL | 0.3983 mL | 0.7965 mL | 1.9913 mL | |
| 40 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4935 mL | |
| 50 mM | 0.0478 mL | 0.2390 mL | 0.4779 mL | 1.1948 mL | |
| 60 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9956 mL | |
| 80 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7467 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2390 mL | 0.5974 mL |
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