1. Search Result
Search Result
Results for "

Pyruvate+dehydrogenase+kinase

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

2

Peptides

8

Recombinant Proteins

3

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-Y0445A
    Sodium dichloroacetate
    Maximum Cited Publications
    26 Publications Verification

    PDK-1 NKCC PDHK Reactive Oxygen Species (ROS) Apoptosis Cancer
    Sodium dichloroacetate is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor. Sodium dichloroacetate also stimulates pyruvate dehydrogenase (PDH) activity and works as a Na +-K +-2Cl cotransporter (NKCC) inhibitor. Sodium dichloroacetate prevents the phosphorylation of the E1α subunit of PDC, promoting the entry of pyruvate into the mitochondria for oxidative metabolism, reducing lactate production, and simultaneously increasing the production of reactive oxygen species (ROS). Sodium dichloroacetate inhibits tumor cell proliferation and induces apoptosis. Sodium dichloroacetate is promising for research of cancers .
    Sodium dichloroacetate
  • HY-135954A
    PDK4-IN-1 hydrochloride
    3 Publications Verification

    PDHK Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    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 .
    PDK4-IN-1 hydrochloride
  • HY-16082
    AZD7545
    4 Publications Verification

    PDHK Metabolic Disease
    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 .
    AZD7545
  • HY-12492
    VER-246608
    4 Publications Verification

    PDHK Cancer
    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.
    VER-246608
  • HY-135954
    PDK4-IN-1
    3 Publications Verification

    PDHK Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    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 .
    PDK4-IN-1
  • HY-121744
    PS10
    5+ Cited Publications

    PDHK Inflammation/Immunology
    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
    PS10
  • HY-136882

    PDHK Cancer
    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 .
    TM-1
  • HY-W005629

    Environmental Pollutants Cannabinoid Receptor PDK-1 Metabolic Disease Cancer
    Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells .
    Leelamine
  • HY-128578
    KPLH1130
    2 Publications Verification

    PDHK NO Synthase Interleukin Related HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    KPLH1130 is a pyruvate dehydrogenase kinase (PDK) inhibitor. KPLH1130 potently inhibits M1 macrophage polarization by reducing the expression of pro-inflammatory cytokines, decreasing the levels of M1 phenotype markers (HIF-1α, iNOS) and nitric oxide (NO) production. KPLH1130 prevents the reduction of mitochondrial oxygen consumption rate (OCR) induced by inflammatory stimuli (LPS ((HY-D1056) + IFN-γ) in various macrophage types. KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 can be used for the study of obesity-associated metabolic disorders and other inflammatory conditions .
    KPLH1130
  • HY-114702
    M77976
    2 Publications Verification

    PDHK Metabolic Disease
    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 .
    M77976
  • HY-149814

    PDHK HSP Cancer
    PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass .
    PDK-IN-1
  • HY-146552

    PDHK Metabolic Disease Cancer
    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 agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-4 has the potential for the research of cancer diseases .
    PDHK-IN-4
  • HY-P10563

    BHV-1100

    CD38 Cancer
    Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .
    Noraramtide
  • HY-157538

    PDHK Cardiovascular Disease
    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-173298

    PDHK Inflammation/Immunology Cancer
    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
  • HY-P3820

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    [Dehydro-Pro4] Substance P (4-11) is a peptide fragment of Substance P. Substance P is a peptide mainly secreted by neurons. Substance P takes part in many biological processes, including nociception, inflammation and immunity .
    [Dehydro-Pro4] Substance P (4-11)
  • HY-173581

    PDHK Cancer
    Arachidonic acid leelamide, a Leelamine (HY-W005629) analog, is a pyruvate dehydrogenase kinase (PDK) inhibitor. Arachidonic acid leelamide can be used for the study of breast cancer .
    Arachidonic acid leelamide
  • HY-146801

    PDHK Metabolic Disease Cancer
    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 .
    PDHK-IN-3
  • HY-162586

    PDHK Cancer
    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-146554

    PDHK Cancer
    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 agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases .
    PDHK-IN-5
  • HY-176008

    Drug Derivative Inflammation/Immunology
    Lauric acid leelamide is the lauric acid (C-12) amide analog of Leelamine (HY-W005629). Leelamine exhibits inhibitory activity against pyruvate dehydrogenase kinase (PDHK) with an IC50 value of 9.5 µM. Leelamine derivatives possess anti-inflammatory effects and can inhibit phospholipase A2 activity from various sources .
    Lauric acid leelamide

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

 

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

 

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: