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PDK

" in MedChemExpress (MCE) Product Catalog:

54

Inhibitors & Agonists

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-117809

    PDK-1 Cancer
    PDK1-IN-2 is a small molecule inhibitor of 3-phosphoinositol-dependent protein kinase-1 (PDK1). PDK1-IN-2 inhibits the binding of PDK1 to its substrate by competitively binding to the PIF pocket of PDK1, thereby inhibiting the kinase activity and downstream signaling of PDK1. PDK1-IN-2 can be used for cell survival and proliferation in cancer .
    PDK1-IN-2
  • HY-157299

    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-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-135954A
    PDK4-IN-1 hydrochloride
    2 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-135954
    PDK4-IN-1
    2 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-W070306

    PDK-1 Neurological Disease Cancer
    PDK1-IN-1 (Compound 2-11) is a PDK1 inhibitor, and can be used for research of myeloproliferative disorders or cancer .
    PDK1-IN-1
  • HY-114645

    PDK-1 Cancer
    PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1 .
    PDK1-IN-RS2
  • HY-156109

    PDHK Mitochondrial Metabolism Cancer
    PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
    PDK-IN-2
  • 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-124288

    Others Others
    PDK1/AurA-IN-1 is an active compound.
    PDK1/AurA-IN-1
  • HY-14440
    MP7
    1 Publications Verification

    PDK1 inhibitor

    PDK-1 Cancer
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
    MP7
  • HY-129426

    Akt Cancer
    PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway .
    PDK1/Akt/Flt dual pathway inhibitor
  • HY-W837864

    Others Others
    PDK1 allosteric modulator 1 is a molecule targeting PDK1 with a binding affinity of 8 μM. PDK1 allosteric modulator 1 is able to bind to the PIF pocket of PDK1, potentially affecting the biological activity of this kinase .
    PDK1 allosteric modulator 1
  • HY-10547
    OSU-03012
    4 Publications Verification

    AR-12; PDK1 inhibitor AR-12

    PDK-1 Autophagy Cancer
    OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM .
    OSU-03012
  • HY-RS10273

    Small Interfering RNA (siRNA) Others

    PDK1 Human Pre-designed siRNA Set A contains three designed siRNAs for PDK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PDK1 Human Pre-designed siRNA Set A
    PDK1 Human Pre-designed siRNA Set A
  • HY-RS10274

    Small Interfering RNA (siRNA) Others

    Pdk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pdk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Pdk1 Mouse Pre-designed siRNA Set A
    Pdk1 Mouse Pre-designed siRNA Set A
  • HY-RS10275

    Small Interfering RNA (siRNA) Others

    Pdk1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pdk1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Pdk1 Rat Pre-designed siRNA Set A
    Pdk1 Rat Pre-designed siRNA Set A
  • HY-RS10276

    Small Interfering RNA (siRNA) Others

    PDK2 Human Pre-designed siRNA Set A contains three designed siRNAs for PDK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PDK2 Human Pre-designed siRNA Set A
    PDK2 Human Pre-designed siRNA Set A
  • HY-RS10277

    Small Interfering RNA (siRNA) Others

    PDK3 Human Pre-designed siRNA Set A contains three designed siRNAs for PDK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PDK3 Human Pre-designed siRNA Set A
    PDK3 Human Pre-designed siRNA Set A
  • HY-RS10278

    Small Interfering RNA (siRNA) Others

    PDK4 Human Pre-designed siRNA Set A contains three designed siRNAs for PDK4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PDK4 Human Pre-designed siRNA Set A
    PDK4 Human Pre-designed siRNA Set A
  • HY-P5450

    PDK-1 Others
    PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)
    PDKtide
  • HY-149275

    Pyruvate Kinase PDK-1 Akt EGFR Apoptosis Cancer
    PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway .
    PKM2/PDK1-IN-1
  • HY-146977

    PDK-1 Cancer
    LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases .
    LDHA/PDKs-IN-1
  • HY-146978

    PDK-1 Cancer
    LDHA/PDKs-IN-2 (compound 20k) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 1.6 and 0.7 μM, respectively. LDHA/PDKs-IN-2 reduces A549 cell proliferation with an EC50 of 15.7 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-2 has the potential for the research of cancer diseases .
    LDHA/PDKs-IN-2
  • HY-12492
    VER-246608
    2 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-121744
    PS10
    2 Publications Verification

    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 [2].PDK: pyruvate dehydrogenase kinase
    PS10
  • HY-W005629

    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-19564
    JX06
    1 Publications Verification

    PDHK Apoptosis Cancer
    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 .
    JX06
  • HY-124060

    PDK-1 Cancer
    PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 .
    PS423
  • HY-121629

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K .
    PS210
  • HY-11005
    BX-912
    4 Publications Verification

    PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
    BX-912
  • HY-13842
    BX517
    1 Publications Verification

    PDK-1 Cancer
    BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
    BX517
  • HY-15967
    PS48
    5 Publications Verification

    PDK-1 Cancer
    PS48 is an activator of PDK1 with an AC50 of 8 μM.
    PS48
  • HY-N6769
    Radicicol
    3 Publications Verification

    Monorden

    HSP Bacterial Antibiotic Parasite Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
    Radicicol
  • HY-14981
    GSK2334470
    5+ Cited Publications

    PDK-1 Cancer
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
    GSK2334470
  • HY-117885

    PDK-1 Cancer
    PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cell proliferation and transformation in breast cancer cells .
    PF-5177624
  • HY-N0047
    Polyphyllin I
    1 Publications Verification

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
    Polyphyllin I
  • HY-13856

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment .
    (R)-PS210
  • HY-W998345

    PROTACs PDK-1 Akt Cancer
    SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
    SMART1
  • HY-N0645
    Dicoumarol
    5+ Cited Publications

    Dicumarol

    PDHK Cancer
    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.
    Dicoumarol
  • HY-13851

    PDK-1 Others
    PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48 .
    PS47
  • HY-128578

    PDHK Metabolic Disease Inflammation/Immunology
    KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice .
    KPLH1130
  • HY-114702
    M77976
    1 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-124379
    TPCK
    1 Publications Verification

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    Ser/Thr Protease HPV Apoptosis PDK-1 Infection Neurological Disease Inflammation/Immunology Cancer
    TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
    TPCK
  • HY-10515

    PDK-1 Cancer
    BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect .
    BX-320
  • HY-116257

    Others Others
    GSK-7227 (compound 32) is a PPARδ partial agonist with the activity of regulating the expression of related genes. GSK-7227 has partial agonist effects on PPARδ target genes CPT1a and PDK4 in skeletal muscle cells.
    GSK-7227
  • HY-135773

    Prostaglandin Receptor PDK-1 Cardiovascular Disease Inflammation/Immunology
    CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist . CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation .
    CRTh2 antagonist 3
  • HY-151465

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
    HIF-1α-IN-4
  • HY-10514
    BX795
    Maximum Cited Publications
    26 Publications Verification

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
    BX795
  • HY-18676B

    OSU-T315 analog

    Integrin Autophagy Apoptosis Caspase PDHK Cancer
    ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models .
    ILK-IN-2

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