2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. PDHK

PDHK

Pyruvate dehydrogenase kinase; PDH kinase

PDHK

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Pyruvate dehydrogenase is a catalyst for an irreversible step in the degradation of glucose and its activity is regulated by a highly specific protein kinase, pyruvate dehydrogenase kinase (PDHK/PDK). PDHK belongs to a family of mitochondrial protein kinases unique from other eukaryotic protein kinases. PDHK inactivates the multienzyme mitochondrial pyruvate dehydrogenase complex by the phosphorylation of three seryl residues in the pyruvate dehydrogenase moiety, and thus plays an important role in the control of glucose homeostasis.

There are four isoforms of PDHK (1 to 4) in humans. PDHK isoforms are up-regulated in obesity, diabetes, heart failure, and cancer and are potential therapeutic targets for these important human diseases.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-157538
    PDK4-IN-2
    		Inhibitor
    PDK4-IN-2 (compound 8) is a pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 of 46 µM. PDK4-IN-2 improves ejection fraction of failing hearts by regulating bioenergetics via activation of the tricarboxylic acid cycle.
    PDK4-IN-2
  • HY-N15518
    Pipcroside C
    		Inhibitor
    Pipcroside C is found in P. crocatum Ruiz & Pav. Pipcroside C is a PDH inhibitor (IC50: 80.25 µM). Pipcroside C has antibacterial activity and is used in the study of oral infections.
    Pipcroside C
  • HY-173301
    PDHK1-IN-3
    		Inhibitor
    PDHK1-IN-3 (Compound 29) is a selective PDHK1 inhibitor with an IC50 of 0.028 μM against PDHK1 and an IC50 of 0.120 μM against PDHK2. PDHK1-IN-3 inhibits the activity of PDHK1 by forming a covalent bond with Lys299 in PDHK1. PDHK1-IN-3 can be used in the research of autoimmune diseases, inflammatory diseases, and cancer.
    PDHK1-IN-3
  • HY-170838
    PDHK1-IN-1
    		Inhibitor
    PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 (IC50=1.5 μM) with anticancer activity. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), limiting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 can shift the metabolism towards an increased glycolysis dependence (Warburg effect). PDHK1-IN-1 can inhibit the phosphorylation of the PDC E1α Ser232 recognition site of PDHK1 and the phosphorylation of Ser293.
    PDHK1-IN-1
  • HY-N15517
    Pipcroside B
    		Inhibitor
    Pipcroside B is found in P. crocatum Ruiz & Pav. Pipcroside B is a PDH inhibitor (IC50: 99.82 µM). Pipcroside B has antibacterial activity and is used in the study of oral infections.
    Pipcroside B
  • HY-162586
    PDHK-IN-7
    		Inhibitor
    PDHK-IN-7 (compound 32) is an inhibitor of pyruvate dehydrogenase kinase with an IC50 value of 17 nM.PDHK-IN-7 activates PDH in rat livers and has a glucose-lowering effect in Zucker fatty rats.
    PDHK-IN-7
  • HY-173298
    PDHK1-IN-2
    		Inhibitor
    PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinases 1/2 (PDHK1/2), with an IC50 of 0.007 μM for PDHK1 and an IC50 of 0.015 μM for PDHK2. PDHK1-IN-2 can regulate immune cell metabolism and correct mitochondrial dysfunction, and is expected to be used in the research of autoimmune diseases, inflammatory diseases, cancers, and other conditions.
    PDHK1-IN-2
Cat. No. Product Name / Synonyms Application Reactivity