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

PDHK

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.

PDHK Related Products (16):

Cat. No. Product Name Effect Purity
  • 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-N0645
    Dicoumarol
    Inhibitor 99.40%
    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 99.91%
    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-19564
    JX06
    Inhibitor 99.88%
    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
  • HY-121744
    PS10
    Inhibitor 99.26%
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
  • HY-W005629
    Leelamine
    Inhibitor 98.36%
    Leelamine is a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity.
  • HY-146552
    PDHK-IN-4
    Inhibitor
    PDHK-IN-4 (Compound 30) is a potent inhibitor of PDHK with IC50s of 0.0051 and 0.0122 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. PDHK-IN-4 has the potential for the research of cancer diseases.
  • HY-136882
    TM-1
    Inhibitor
    TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation.
  • HY-12492
    VER-246608
    Inhibitor 98.92%
    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-135954A
    PDK4-IN-1 hydrochloride
    Inhibitor 99.48%
    PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
  • HY-114702
    M77976
    Inhibitor 99.63%
    M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes.
  • HY-128578
    KPLH1130
    Inhibitor 99.95%
    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-135954
    PDK4-IN-1
    Inhibitor
    PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
  • HY-146801
    PDHK-IN-3
    Inhibitor
    PDHK-IN-3 (compound 7) is a potent PDHK (pyruvate dehydrogenase kinase) inhibitor, with IC50 values of 0.21 and 1.54 μM for PDHK2 and PDHK4, respectively.
  • HY-N0645S
    Dicoumarol-d8
    Inhibitor
    Dicoumarol-d8 (Dicumarol-d8) is the deuterium labeled Dicoumarol. 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-146554
    PDHK-IN-5
    Inhibitor
    PDHK-IN-5 (Compound 19) is a potent inhibitor of PDHK with IC50s of 0.006 and 0.0329 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases.