GSK2194069
Based on 5 publication(s) in Google Scholar
GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively.
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- Pureza: 99.80%
- No. CAS: 1332331-08-4
- Fòrmula: C25H24N4O3
- Peso molecular:428.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GSK2194069
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Actividad biológica
GSK2194069 (100 nM; 24 h) inhibits fatty acid synthase (FAS) in cancer cell lines (KATO-III, MKN45, A549, SNU-1) without reducing FAS production protein level[1].
GSK2194069 decreases phosphatidylcholine levels in A549 cells with a half-maximum effective concentration (EC50) value of 15.5 ± 9 nM (n = 78), correlating with the decreased palmitate synthesis[1].
GSK2194069 (5 μM and 20 μM) shows higher efficacy in FASN-positive LNCaP cells rather than FASN-negative PC3 cells, with the higher FASN Expression level in LNCaP cells[2].
GSK2194069 (50 μM; 24 h) inhibits the growth of LNCaP-LN3 human prostate cancer cells[3].
GSK2194069 (60.4 nM; 24 h) displays properties of metabolomics, including L-acetyl carnitine, stearoyl carnitine, vaccenyl carnitine, and palmitoyl-L-carnitine decrease in LNCaP-LN3 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549
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Concentration:0, 10, 100, 1000 nM
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Incubation Time:48 hours or 120 hours
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Result:Didn’t decrease FAS protein level.
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Cell Line:FASN-positive LNCaP cells, and FASN-negative PC3 cells
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Concentration:1 nM-0.1 mM
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Incubation Time:48 hours
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Result:Inhibited tumor cells growth significantly, and reduced LNCaP cells much better.
Chemical Information
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No. CAS 1332331-08-4
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Appearance Solid
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Peso molecular 428.48
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Fòrmula C25H24N4O3
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Color Light yellow to brown
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SMILES
O=C(N1C[C@H](CC2=NNC(N2C3=CC=C(C4=CC=C(OC=C5)C5=C4)C=C3)=O)CC1)C6CC6
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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 (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Anal Chem
Molecular Imaging and In Situ Quantitative Profiling of Fatty Acid Synthase with a Chemical Probe. [Abstract]2020 Mar 17;92(6):4419-4426. PMID: 32053360 -
ACS Omega
Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]2024 Feb 28;9(10):11870-11882. PMID: 38496939 -
PLoS One
Feedback activation of AMPK-mediated autophagy acceleration is a key resistance mechanism against SCD1 inhibitor-induced cell growth inhibition. [Abstract]2017 Jul 13;12(7):e0181243. PMID: 28704514 -
bioRxiv
SCD1 and SCD5 Modulate PARP-Dependent DNA Repair via Fatty Acid Desaturation in Glioblastoma. [Abstract]2025 Jul 27:2025.07.23.666454. PMID: 40777251
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (233.38 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 (5.83 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.83 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hardwicke MA, et al. A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol. 2014 Sep;10(9):774-9. [Content Brief]
[2]. Kelly JM, et al. Synthesis and Evaluation of 11C-Labeled Triazolones as Probes for Imaging Fatty Acid Synthase Expression by Positron Emission Tomography. Molecules. 2022 Feb 25;27(5):1552. [Content Brief]
[3]. Oh JE, et al. Deciphering Fatty Acid Synthase Inhibition-Triggered Metabolic Flexibility in Prostate Cancer Cells through Untargeted Metabolomics. Cells. 2020 Nov 10;9(11):2447. [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 | 2.3338 mL | 11.6692 mL | 23.3383 mL | 58.3458 mL |
| 5 mM | 0.4668 mL | 2.3338 mL | 4.6677 mL | 11.6692 mL | |
| 10 mM | 0.2334 mL | 1.1669 mL | 2.3338 mL | 5.8346 mL | |
| 15 mM | 0.1556 mL | 0.7779 mL | 1.5559 mL | 3.8897 mL | |
| 20 mM | 0.1167 mL | 0.5835 mL | 1.1669 mL | 2.9173 mL | |
| 25 mM | 0.0934 mL | 0.4668 mL | 0.9335 mL | 2.3338 mL | |
| 30 mM | 0.0778 mL | 0.3890 mL | 0.7779 mL | 1.9449 mL | |
| 40 mM | 0.0583 mL | 0.2917 mL | 0.5835 mL | 1.4586 mL | |
| 50 mM | 0.0467 mL | 0.2334 mL | 0.4668 mL | 1.1669 mL | |
| 60 mM | 0.0389 mL | 0.1945 mL | 0.3890 mL | 0.9724 mL | |
| 80 mM | 0.0292 mL | 0.1459 mL | 0.2917 mL | 0.7293 mL | |
| 100 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5835 mL |
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