M77976
Based on 2 publication(s) in Google Scholar
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes.
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- Pureza: 99.44%
- No. CAS: 394237-61-7
- Fòrmula: C17H16N2O3
- Peso molecular:296.32
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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) M77976
More
Actividad biológica
IC50: 648 μM (PDK4)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | GI50 |
33.3 μM
Compound: 4
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Inhibitory concentration against cell proliferation of human HCT116 cells
Inhibitory concentration against cell proliferation of human HCT116 cells
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[PMID: 15974572] |
M77976 binds to the ATP-binding pocket of PDK4 and causes local conformational changes with complete disordering of the ATP lid[1].
M77976 makes hydrophobic interactions with the side chains of Asn258, Ala262, Val298, Leu306 and Thr358 of PDK4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 394237-61-7
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Appearance Solid
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Peso molecular 296.32
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Fòrmula C17H16N2O3
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Color White to off-white
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SMILES
COC1=CC=C(C=C1)C2=C(NN=C2C3=CC=C(C=C3O)O)C
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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 (2)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Ginsenoside Rg3 antagonises endometriosis glycolysis via the tripartite motif containing 28 and pyruvate dehydrogenase kinase 4 signalling pathway. [Abstract]2026 Feb:151:157792. PMID: 41539092 -
Cancer Metab
Deficiency of TOP1MT enhances glycolysis through the stimulation of PDK4 expression in gastric cancer. [Abstract]2024 Jan 10;12(1):2. PMID: 38200513
Solvente y solubilidad
DMSO : 250 mg/mL (843.68 mM; Need ultrasonic; 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, 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: ≥ 2.08 mg/mL (7.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.3747 mL | 16.8736 mL | 33.7473 mL | 84.3682 mL |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | 16.8736 mL | |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL | 8.4368 mL | |
| 15 mM | 0.2250 mL | 1.1249 mL | 2.2498 mL | 5.6245 mL | |
| 20 mM | 0.1687 mL | 0.8437 mL | 1.6874 mL | 4.2184 mL | |
| 25 mM | 0.1350 mL | 0.6749 mL | 1.3499 mL | 3.3747 mL | |
| 30 mM | 0.1125 mL | 0.5625 mL | 1.1249 mL | 2.8123 mL | |
| 40 mM | 0.0844 mL | 0.4218 mL | 0.8437 mL | 2.1092 mL | |
| 50 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6874 mL | |
| 60 mM | 0.0562 mL | 0.2812 mL | 0.5625 mL | 1.4061 mL | |
| 80 mM | 0.0422 mL | 0.2109 mL | 0.4218 mL | 1.0546 mL | |
| 100 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8437 mL |
M77976 Related Classifications
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