TM-1
Based on 1 Customer Validation
TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation.
For research use only. We do not sell to patients.
- Purity: 99.05%
- CAS No.: 921099-13-0
- Formula: C26H32N2O6
- Molecular Weight:468.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 2.97 μM (PDK1), 5.2 μM (PDK2)[1]
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Cell Line
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Type | Value | Description | References |
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| MG-63 | EC50 |
14.5 μM
Compound: TM-1
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Anti-proliferative activity against human MG63 cells after 72 hrs by MTT assay
Anti-proliferative activity against human MG63 cells after 72 hrs by MTT assay
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[PMID: 29150396] |
TM-1 (0-10 μM) inhibits PDHK1 activity with the inhibition rate of 80.5% (dosage at 10 μM) and an IC50 value of 2.97 μM[1].
TM-1 (0-2.1 μM; 12 h) shows anti-osteosarcoma activity and inhibits MG-63 cells with an EC50 value of 14.5 μM[1].
TM-1 (3, 6, 12 μM; 24 h) decreases PDHC phosphorylation of both Ser293 and Ser232 sites in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MG-63 cells
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Concentration:3, 6, 12 μM
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Incubation Time:24 hours
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Result:Dramatically reduced the PDHK phosphorylation of both Ser293 and Ser232 sites at 6 or 12 μM.
Chemical Information
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CAS No. 921099-13-0
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Appearance Solid
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Molecular Weight 468.54
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Formula C26H32N2O6
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Color Off-white to light brown
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SMILES
O=C1C(C2=CC=C(OC)C(OC)=C2)=C(C)C3=CC=C(OCCN4CCN(CCO)CC4)C=C3O1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (106.71 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, 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.
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: ≥ 1.25 mg/mL (2.67 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.67 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Purity & Documentation
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Data Sheet (269 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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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 | 2.1343 mL | 10.6714 mL | 21.3429 mL | 53.3572 mL |
| 5 mM | 0.4269 mL | 2.1343 mL | 4.2686 mL | 10.6714 mL | |
| 10 mM | 0.2134 mL | 1.0671 mL | 2.1343 mL | 5.3357 mL | |
| 15 mM | 0.1423 mL | 0.7114 mL | 1.4229 mL | 3.5571 mL | |
| 20 mM | 0.1067 mL | 0.5336 mL | 1.0671 mL | 2.6679 mL | |
| 25 mM | 0.0854 mL | 0.4269 mL | 0.8537 mL | 2.1343 mL | |
| 30 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7786 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3339 mL | |
| 50 mM | 0.0427 mL | 0.2134 mL | 0.4269 mL | 1.0671 mL | |
| 60 mM | 0.0356 mL | 0.1779 mL | 0.3557 mL | 0.8893 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5336 mL |
TM-1 Related Classifications
HY-136882 Related Classifications
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