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

PDHK

Pyruvate dehydrogenase (PDH) is a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDH kinase; PDHK; PDK) results in inactivation. Multiple alternatively spliced transcript variants have been found for this gene. PDH catalyzes the conversion of pyruvate to acetyl-coenzyme A, which enters into the Krebs cycle, providing ATP to the cell. PDH activity is under the control of pyruvate dehydrogenase kinases (PDHKs).

PDHK Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-12492
    VER-246608 Inhibitor 99.03%
    VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
  • HY-N0645
    Dicoumarol Inhibitor 98.70%
    Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.
  • HY-16082
    AZD7545 Inhibitor 99.84%
    AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
  • HY-128578
    KPLH1130 Inhibitor 99.53%
    KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.
  • HY-Y0445A
    Sodium dichloroacetate Inhibitor >98.0%
    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
  • HY-121744
    PS10 Inhibitor
    PS10 is a novel, potent and selective PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM and 0.76 μM for PDK2 and PDK4, respectively. PS10 improves lucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy. PDK: pyruvate dehydrogenase kinase
Isoform Specific Products

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