PDK1-IN-5
PDK1-IN-5 is a selective PDK1 inhibitor. PDK1-IN-5 activaties PDH by diminishing phosphorylation level via PDK1 inhibition. PDK1-IN-5 effectively reverses the Warburg effect and shifts cellular energy metabolism from glycolysis toward oxidative phosphorylation by increased acetyl-CoA, reduced lactate, elevated mitochondrial ROS, and subsequent induction of apoptosis. PDK1-IN-5 robustly inhibits tumor growth in vivo without inducing systemic toxicity. PDK1-IN-5 can be used for lung adenocarcinoma, human non-small cell lung adenocarcinoma and gastric colorectal.
For research use only. We do not sell to patients.
- Formula: C16H12Cl2F3NO3
- Molecular Weight:394.17
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
PDK1-IN-5 (compound D16) (48 h) shows selectivity and superior antiproliferative activity in A549 (lung adenocarcinoma), PC9 (lung adenocarcinoma), H1975 (human non-small cell lung adenocarcinoma), HGC-27 (gastric), and HCT-116 (colorectal) with IC50s of 0.86, 5.99, 4.92, 2.48 and 1.15 μM, respectively[1].
PDK1-IN-5 (1μM) exhibits strong PDK1 inhibitory activity with inhibiton = 53.20%[1].
PDK1-IN-5 (0-12 μM, 0.5 h) activates PDH by diminishing the phosphorylation level of PDH via inhibition of PDK1 activity in A549 and PC9 cells[1].
PDK1-IN-5 (0.4-1.6 μM, 14 days) suppresses a concentration-dependent proliferative capacity in A549 and PC9 cells[1].
PDK1-IN-5 (0.4-1.6 μM and 3-12 μM, 24 h) inhibits cellular migration of both A549 and PC9 cells in a dose-dependent fashion[1].
PDK1-IN-5 (0.2-3.2 μM and 1.5-24 μM, 48 h) elevates mitochondrial ROS levels and induces concentration-dependent apoptosis[1].
PDK1-IN-5 (0.2-3.2 μM and 1.5-24 μM, 24 and 48 h) effectively changes tumor cell metabolism by reversing the Warburg effect through potent PDK1 inhibition, shifting the energy balance from glycolysis toward OXPHOS and highlighting its therapeutic potential[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and PC9 cells
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Concentration:0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
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Incubation Time:0.5 h
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Result:Decreased the expression of phosphorylated protein pPDH (serine 293) in a concentration-dependent manner.
Reduced phosphorylation level and raised PDHA1 expression.
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Cell Line:A549 and PC9 cells
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Concentration:0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
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Incubation Time:14 days
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Result:Achieved 98 % inhibition of colony formation at 14 day in high concentration treatment (1.6 μM).
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Cell Line:A549 and PC9 cells
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Concentration:0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
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Incubation Time:24 h
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Result:Reached 80.5 % inhibition at the highest concentration.
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Cell Line:A549 and PC9 cells
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Concentration:0.2, 0.8 and 3.2 μM (A549); 1.5, 6, 24 μM (PC9)
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Incubation Time:48 h
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Result:Induced PC9 cells apoptotic rate at 1.5, 6, and 24 μM with 7.0%, 12.5%, and 17.7%, respectively.
Induced A549 cells apoptotic rate at 0.2, 0.8, and 3.2 μM with 16.1%, 26.6%, and 30.7%, respectively.
| Species | Dose | Route | T1/2 | Cmax | AUC0-∞ | AUC0-t | MRT0-∞ | Vz | CL |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 1.56 h | 1.12 μg/mL | 0.85 μg·h/mL | 0.84 μg·h/mL | 0.95 h | 13.55 L/kg | 5.94 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c-nu nude mice (4 weeks old) were implanted with A549 and PC9 cells[1].
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Dosage:5, 10, and 20 mg/kg
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Administration:i.p., every 2 days for 14 days
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Result:Revealed no pathological abnormalities in Hematoxylin-Eosin (H&E) in major organs (heart, liver, spleen, lung, kidney) from the 20 mg/kg.
Maintained stable body weights in animals throughout the experimental period.
Downregulated PDK1 expression and reduced the number of Ki-67-positive cells in treated tumors.
Chemical Information
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Molecular Weight 394.17
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Formula C16H12Cl2F3NO3
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SMILES
O=C(NC1=CC=C(OCC2=CC=C(OC(F)(F)F)C=C2)C=C1)C(Cl)Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDK1-IN-5 Related Classifications
HY-179501 Related Classifications
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