2. PI3K/Akt/mTOR NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. PDK-1 Reactive Oxygen Species (ROS) Apoptosis Oxidative Phosphorylation
  4. 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.

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PDK1-IN-5

PDK1-IN-5 Chemical Structure

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PDK1-IN-5 Related Antibodies

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Description

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[1].

In Vitro

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.

PDK1-IN-5 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 and PC9 cells
Concentration: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
Incubation Time: 0.5 h
Result: Decreased the expression of phosphorylated protein pPDH (serine 293) in a concentration-dependent manner.
Reduced phosphorylation level and raised PDHA1 expression.

Cell Proliferation Assay[1]

Cell Line: A549 and PC9 cells
Concentration: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
Incubation Time: 14 days
Result: Achieved 98 % inhibition of colony formation at 14 day in high concentration treatment (1.6 μM).

Cell Migration Assay [1]

Cell Line: A549 and PC9 cells
Concentration: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
Incubation Time: 24 h
Result: Reached 80.5 % inhibition at the highest concentration.

Cell Cytotoxicity Assay[1]

Cell Line: A549 and PC9 cells
Concentration: 0.2, 0.8 and 3.2 μM (A549); 1.5, 6, 24 μM (PC9)
Incubation Time: 48 h
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.
Parmacokinetics
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
In Vivo

PDK1-IN-5 (compound D16) (5-20 mg/kg, i.p., every 2 days for 14 days) exerts anti-tumor effects in vivo through inhibition of tumor proliferation in A549 and PC9 xenograft mouse models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c-nu nude mice (4 weeks old) were implanted with A549 and PC9 cells[1].
Dosage: 5, 10, and 20 mg/kg
Administration: i.p., every 2 days for 14 days
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.
Molecular Weight

394.17

Formula

C16H12Cl2F3NO3
SMILES

O=C(NC1=CC=C(OCC2=CC=C(OC(F)(F)F)C=C2)C=C1)C(Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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PDK1-IN-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PDK1-IN-5PDK-1Reactive Oxygen Species (ROS)ApoptosisOxidative Phosphorylation3-Phosphoinositide-dependent protein kinase 1PDK1PDHWarburg effectacetyl-CoAROSapoptosislung adenocarcinomahuman non-small cell lung adenocarcinoma and gastric colorectal.Inhibitorinhibitorinhibit

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