PDK4-IN-1
Based on 3 publication(s) in Google Scholar
PDK4-IN-1 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 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
For research use only. We do not sell to patients.
- Purity: 99.34%
- CAS No.: 2310262-10-1
- Formula: C22H19N3O2
- Molecular Weight:357.41
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Publications Citing Use of MedChemExpress (MCE) PDK4-IN-1
More
Biological Activity
IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))[1]
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. 2310262-10-1
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Appearance Solid
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Molecular Weight 357.41
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Formula C22H19N3O2
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Color Light yellow to yellow
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SMILES
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 and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (279.79 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 and light). 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 and light). 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)
Purity & Documentation
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Data Sheet (281 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
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 and light). 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 | 2.7979 mL | 13.9895 mL | 27.9791 mL | 69.9477 mL |
| 5 mM | 0.5596 mL | 2.7979 mL | 5.5958 mL | 13.9895 mL | |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7979 mL | 6.9948 mL | |
| 15 mM | 0.1865 mL | 0.9326 mL | 1.8653 mL | 4.6632 mL | |
| 20 mM | 0.1399 mL | 0.6995 mL | 1.3990 mL | 3.4974 mL | |
| 25 mM | 0.1119 mL | 0.5596 mL | 1.1192 mL | 2.7979 mL | |
| 30 mM | 0.0933 mL | 0.4663 mL | 0.9326 mL | 2.3316 mL | |
| 40 mM | 0.0699 mL | 0.3497 mL | 0.6995 mL | 1.7487 mL | |
| 50 mM | 0.0560 mL | 0.2798 mL | 0.5596 mL | 1.3990 mL | |
| 60 mM | 0.0466 mL | 0.2332 mL | 0.4663 mL | 1.1658 mL | |
| 80 mM | 0.0350 mL | 0.1749 mL | 0.3497 mL | 0.8743 mL | |
| 100 mM | 0.0280 mL | 0.1399 mL | 0.2798 mL | 0.6995 mL |
PDK4-IN-1 Related Classifications
HY-135954 Related Classifications
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