PS10
Based on 6 publication(s) in Google Scholar
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
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- Purity: 98.51%
- CAS No.: 1564265-82-2
- 화학식: C14H13NO6S
- 분자량:323.32
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PS10
More
Biological Activity
IC50: 0.8 μM (PDK2); 0.76 μM (PDK4); 2.1 μM (PDK3); 21.3 μM (PDK1)[1]
PS10 shows a higher affinity of PS10 for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47,000 nM)[1].PS10 is less potent than cycloheximide in HeLa cells, it shows an IC50 value of 284 μM for the growth inhibition and PS10 has low toxicity in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J male mice at 6 to 8 weeks old[2]
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Dosage:70 mg/kg/day
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Administration:Intraperitoneal injection
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Result:Improved glucose tolerance in the intact animal.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1564265-82-2
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Appearance Solid
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분자량 323.32
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화학식 C14H13NO6S
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Color Light yellow to khaki
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SMILES
OC1=CC(O)=CC2=C1CN(S(=O)(C3=CC=C(O)C=C3O)=O)C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Metab
2025 Apr;7(4):823-841. PMID: 40275022 -
Int J Biol Macromol
Targeting the PDK/PDH axis to reverse metabolic abnormalities by structure-based virtual screening with in vitro and in vivo experiments. [Abstract]2024 Feb 6;262(Pt 1):129970. PMID: 38325689 -
Biomedicines
2022 Dec 7;10(12):3171. PMID: 36551928 -
J Virol
Small-molecule PS10 inhibits PRRSV replication by targeting HSP90 and multiple viral non-structural proteins. [Abstract]2026 Mar 24;100(3):e0212125. PMID: 41705837 -
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용액&용해도
DMSO : 62.5 mg/mL (193.31 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: ≥ 6.25 mg/mL (19.33 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (19.33 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.J Biol Chem. 2014 Feb 14;289(7):4432-43. [Content Brief]
[2]. Wu CY, et al. A novel inhibitor of pyruvate dehydrogenase kinase stimulates myocardial carbohydrate oxidation in diet-induced obesity.J Biol Chem. 2018 Jun 22;293(25):9604-9613. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0929 mL | 15.4646 mL | 30.9291 mL | 77.3228 mL |
| 5 mM | 0.6186 mL | 3.0929 mL | 6.1858 mL | 15.4646 mL | |
| 10 mM | 0.3093 mL | 1.5465 mL | 3.0929 mL | 7.7323 mL | |
| 15 mM | 0.2062 mL | 1.0310 mL | 2.0619 mL | 5.1549 mL | |
| 20 mM | 0.1546 mL | 0.7732 mL | 1.5465 mL | 3.8661 mL | |
| 25 mM | 0.1237 mL | 0.6186 mL | 1.2372 mL | 3.0929 mL | |
| 30 mM | 0.1031 mL | 0.5155 mL | 1.0310 mL | 2.5774 mL | |
| 40 mM | 0.0773 mL | 0.3866 mL | 0.7732 mL | 1.9331 mL | |
| 50 mM | 0.0619 mL | 0.3093 mL | 0.6186 mL | 1.5465 mL | |
| 60 mM | 0.0515 mL | 0.2577 mL | 0.5155 mL | 1.2887 mL | |
| 80 mM | 0.0387 mL | 0.1933 mL | 0.3866 mL | 0.9665 mL | |
| 100 mM | 0.0309 mL | 0.1546 mL | 0.3093 mL | 0.7732 mL |
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