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Results for "

Pyruvate dehydrogenase kinase

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

1

Natural
Products

8

Recombinant Proteins

2

Antibodies

Targets Recommended:
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
    TM-1

    		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-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-W005629
    Leelamine

    		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-149814
    PDK-IN-1

    		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-148062
    RSS0680

    		PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK Others
    RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC with protein kinase degradation activity (Pink: FLT3-IN-17 (HY-148070); Black: Linker (HY-W041970); Blue: E3 ligase Ligand (HY-112078)). RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
    RSS0680
  • HY-157299
    PDK-IN-3

    		PDHK Cancer
    PDK-IN-3 (compound 1) is a potent pan inhibitor of PDK with IC50s of 109.3, 135.8, 458.7 nM and 8.67 μM against PDK 1-4, respectively. PDK-IN-3 also induces proliferation and apoptosis in A549 cells .
    PDK-IN-3
  • HY-146552
    PDHK-IN-4

    		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-157538
    PDK4-IN-2

    		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-W134163
    (E)-2-Octenal

    trans-2-Octenal

    		 Fungal Reactive Oxygen Species (ROS) Mitochondrial Metabolism Phosphatase Pyruvate Kinase Infection
    (E)-2-Octenal is an Antifungal agent. (E)-2-Octenal disrupts cell membrane integrity and causes ROS accumulation. (E)-2-Octenal decreases the activities of phosphofructokinase and pyruvate kinase. (E)-2-Octenal inhibits Neofusicoccum parvum growth by disrupting mitochondrial energy metabolism. (E)-2-Octenal suppresses the growth of a Prochloraz (HY-B0845)-resistant Penicillium italicum strain. (E)-2-octenal exerts a broad-spectrum and potent inhibitory effect on various fungi, including Sclerotium rolfsii, Metarhizium anisopliae sensu lato, and Aspergillus flavus, etc. (E)-2-Octenal can be used for the research of citrus blue mold and mango stem-end rot .
    (E)-2-Octenal
  • HY-173298
    PDHK1-IN-2

    		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-146801
    PDHK-IN-3

    		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-123650
    FSBA hydrochloride

    5'-p-Fluorosulfonylbenzoyladenosine

    		 Biochemical Assay Reagents Cancer
    FSBA (5'-p-Fluorosulfonylbenzoyladenosine) hydrochloride is a covalent modifier and affinity labeling reagent for adenine nucleotide-binding proteins. FSBA hydrochloride covalently attaches to the nucleotide-binding sites of pyruvate kinase, glutamate dehydrogenase, and p56 lck, and to a lysine residue in the ATP-binding site of cAMP-dependent protein kinase, causing loss of enzymatic activity. FSBA hydrochloride can be used for the research of T lymphoma .
    FSBA hydrochloride
  • HY-E70953
    Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit

    		Pyruvate Kinase Lactate Dehydrogenase Metabolic Disease
    Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit catalyzes an ATP-dependent phosphorylation of glycolate to yield 2-phosphoglycolate. Pyruvate kinase requires bivalent and monovalent cations such as Mg 2+ and K + respectively for activation to occur.
    Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit
  • HY-173581
    Arachidonic acid leelamide

    		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-162586
    PDHK-IN-7

    		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-IN-5

    		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
    Lauric acid leelamide

    		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
  • HY-182037
    Multi-target kinase-IN-9

    		DNA/RNA Synthesis Pyruvate Kinase Cancer
    Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research .
    Multi-target kinase-IN-9

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