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PDK

In the field of biochemistry, PDPK1 refers to the protein 3-phosphoinositide-dependent protein kinase-1, an enzyme which is encoded by the PDPK1 gene in humans. It is implicated in the development and progression of melanomas.PDPK1 is a master kinase, which is crucial for the activation of AKT/PKB and many other AGC kinases including PKC, S6K, SGK. An important role for PDPK1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling.

  • MP7
    T123981001409-50-2In house
    MP7 (PDK1 inhibitor) is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
    • $45
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  • Sodium dichloroacetate
    T36042156-56-1
    Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.
    • $31
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    TargetMol | Citations Cited
  • RS1-PDK1 inhibitor
    T247411643958-85-3In house
    RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders.
    • $350
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  • 6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile
    T776851207836-10-9
    6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study angiosarcoma, adenocarcinoma, multiple myeloma, psoriasis, prostate cancer, and Alzheimer's disease.
    • $30
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    TargetMol | Inhibitor Sale
  • M77976
    T15944394237-61-7In house
    M77976 is a selective ATP-competitive inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an inhibitory effect on PDK4, having an IC50 value of 648 μM. It is used for research related to obesity and diabetes.
    • $43
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    TargetMol | Inhibitor Sale
  • VER-246608
    T172241684386-71-7
    VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytosta
    • $48
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  • BX-912
    T1837702674-56-4
    BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.
    • $48
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  • PDK1-IN-RS2
    T164501643958-89-7
    PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM).
    • $183
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  • Rabusertib
    T6084911222-45-2
    Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.
    • $38
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    TargetMol | Citations Cited
  • KPLH1130
    T11765906669-07-6
    KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.
    • $76
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  • PS10
    T125661564265-82-2
    PS10 is a ATP-competitive inhibitor of pan-PDK(PDK2, PDK4, PDK1, and PDK3 with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM , respectively).
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    • PS47
      T246771180676-33-8
      PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.
      • $32
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    • BX795
      T1830702675-74-9
      BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
      • $54
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    • JX06
      T22350729-46-4
      JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.
      • $43
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    • PS 48
      T31631180676-32-7
      PS 48 has been shown to be a PKB Kinase (PDK1) activator (Kd: 10.3 μM). This compound selectively binds to the PIF-binding pocket of PKB Kinase (PDK1).
      • $47
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    • BX517
      T4046850717-64-5
      BX517 (PDK1 inhibitor 2) is a potent and selective inhibitor of PDK1.
      • $31
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    • Osu03012
      T2466742112-33-0
      Osu03012 (AR-12) is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity.
      • $31
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      TargetMol | Citations Cited
    • Polyphyllin I
      T389550773-41-6
      Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.
      • $52
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      TargetMol | Citations Cited
    • PDK4-IN-1 hydrochloride
      T12412L2310262-11-2
      PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM)
      • $129
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    • δ-Tocotrienol
      TMA247425612-59-3
      δ-Tocotrienol (Delta-Tocotrienol) is a potential angiogenic inhibitor. δ-Tocotrienol is also a nontoxic activator of mir-34a which can inhibit nonsmall cell lung cancer cells (NSC-LC) cell proliferation, induce apoptosis and inhibit invasion, and thus offering a potential starting point for the design of novel anticancer agents.
      • $59
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    • PS210
      T166701221962-86-2
      PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves as a substrate-selective inhibitor of PDK1 in cells, inhibiting the phosphorylation and activation of S6K.
      • $31
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    • PHT-427
      T24201191951-57-1
      PHT-427 (CS-0223) is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
      • $39
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      TargetMol | Citations Cited
    • GSK2334470
      T23481227911-45-6
      GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
      • $48
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    • Dehydroabiethylamine
      T197831446-61-3
      Dehydroabiethylamine (NSC-2955) is an inducer of hepatic CYP2B activity. Dehydroabiethylamine inhibits pyruvate dehydrogenase kinases (PDKs) and intracellular cholesterol transport with anti-tumor activity.
      • $39
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    • Dicoumarol
      T080966-76-2
      Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.
      • $41
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