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-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 E1伪 Ser232 recognition site of PDHK1 and the phosphorylation of Ser293.
    PDHK1-IN-1
  • 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
Cat. No. Product Name / Synonyms Application Reactivity