PDK4-IN-1 hydrochloride
Based on 3 publication(s) in Google Scholar
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 2310262-11-2
- Formula: C22H20ClN3O2
- Molecular Weight:393.87
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-diabetic Compound Library
HY-L040
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Glycolysis Compound Library
HY-L058
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Orally Active Compound Library
HY-L061
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Anti-Cancer Metabolism Compound Library
HY-L083
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Mitochondria-Targeted Compound Library
HY-L089
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Glucose Metabolism Compound Library
HY-L092
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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TCA Cycle Compound Library
HY-L148
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Cell Death Library
HY-L162
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Lactic Acid Metabolic Compound Library
HY-L204
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) PDK4-IN-1 hydrochloride
More
Biological Activity
IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
36.02 μM
Compound: 8c
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Cytotoxicity against CHOK1 cells
Cytotoxicity against CHOK1 cells
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[PMID: 30623649] |
| HFL1 | IC50 |
36.54 μM
Compound: 8c
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Cytotoxicity against HFL1 cells
Cytotoxicity against HFL1 cells
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[PMID: 30623649] |
| L929 | IC50 |
35.82 μM
Compound: 8c
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Cytotoxicity against mouse L929 cells
Cytotoxicity against mouse L929 cells
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[PMID: 30623649] |
| NIH3T3 | IC50 |
39.64 μM
Compound: 8c
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Cytotoxicity against mouse NIH/3T3 cells
Cytotoxicity against mouse NIH/3T3 cells
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[PMID: 30623649] |
| Vero | IC50 |
36.42 μM
Compound: 8c
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Cytotoxicity against African green monkey Vero cells
Cytotoxicity against African green monkey Vero cells
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[PMID: 30623649] |
PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1[1].
PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis[1].
PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α[1].
10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells[1].
PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and RKO cells
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Concentration:50 μM
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Incubation Time:0 hour, 24 hours, 48 hours, 72hours
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Result:Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.
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Cell Line:HCT116 and RKO cells
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Concentration:10 μM, 25 μM, 50 μM
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Incubation Time:24 hours
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Result:Dose-dependently increased apoptosis.
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Cell Line:HEK293T human embryonic kidney cells
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Inhibited phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α.
Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs[1].
The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (8-week old) fed with high-fat diet[1]
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Dosage:100 mg/kg
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Administration:Oral administration; daily; for 1 week
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Result:Significantly improved glucose tolerance.
Chemical Information
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CAS No. 2310262-11-2
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Appearance Solid
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Molecular Weight 393.87
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Formula C22H20ClN3O2
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Color Light yellow to yellow
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SMILES
[H]Cl.O=C1C2=C(C=CC=C2)C(C3=CC=CC(C4=CN(C5CCNCC5)N=C4)=C13)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Aging Cell
2023 Apr;22(4):e13800. PMID: 36797808 -
Biochem Pharmacol
Targeting PDK4 attenuates neointimal hyperplasia and regulates VSMC phenotypic switching, apoptosis, and autophagy. [Abstract]2026 Feb 12:247:117805. PMID: 41687829 -
Solvent & Solubility
DMSO : 100 mg/mL (253.89 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.08 mg/mL (5.28 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 (5.28 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (282 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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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 (sealed storage, away from moisture). 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 | 2.5389 mL | 12.6945 mL | 25.3891 mL | 63.4727 mL |
| 5 mM | 0.5078 mL | 2.5389 mL | 5.0778 mL | 12.6945 mL | |
| 10 mM | 0.2539 mL | 1.2695 mL | 2.5389 mL | 6.3473 mL | |
| 15 mM | 0.1693 mL | 0.8463 mL | 1.6926 mL | 4.2315 mL | |
| 20 mM | 0.1269 mL | 0.6347 mL | 1.2695 mL | 3.1736 mL | |
| 25 mM | 0.1016 mL | 0.5078 mL | 1.0156 mL | 2.5389 mL | |
| 30 mM | 0.0846 mL | 0.4232 mL | 0.8463 mL | 2.1158 mL | |
| 40 mM | 0.0635 mL | 0.3174 mL | 0.6347 mL | 1.5868 mL | |
| 50 mM | 0.0508 mL | 0.2539 mL | 0.5078 mL | 1.2695 mL | |
| 60 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0579 mL | |
| 80 mM | 0.0317 mL | 0.1587 mL | 0.3174 mL | 0.7934 mL | |
| 100 mM | 0.0254 mL | 0.1269 mL | 0.2539 mL | 0.6347 mL |
PDK4-IN-1 hydrochloride Related Classifications
HY-135954A Related Classifications
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