2. Signaling Pathways
  3. PI3K/Akt/mTOR
  4. PDK-1

PDK-1

3-Phosphoinositide-dependent protein kinase 1

PDK-1

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PDK-1 (3-Phosphoinositide-dependent protein kinase 1), a member of the protein A, G and C (AGC) family of proteins, is a Ser/Thr protein kinase. PDK-1, is the pivotal node in the PI3K pathway, has a key role in insulin and growth-factor signalling through phosphorylation and subsequent activation of a number of other AGC kinase family members, such as protein kinase B.

PDK-1 is responsible for the regulation of cell proliferation and migration and it also has been found to play a key role in different cancers, pancreatic and breast cancer amongst others. Many cancer-driving mutations induce activation of PDK-1 targets including Akt, S6K (p70 ribosomal S6 kinase) and SGK. Thus, PDK1 is a critical activator of multiple pro-survival and oncogenic protein kinases, for which it has garnered considerable interest as an oncology drug target.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-Y0445A
    Sodium dichloroacetate
    		Inhibitor 99.78%
    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-10514
    BX795
    		Inhibitor 99.84%
    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-14981
    GSK2334470
    		Inhibitor 99.79%
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
    GSK2334470
  • HY-N0047
    Polyphyllin I
    		Inhibitor 99.89%
    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-15967
    PS48
    		Activator 99.71%
    PS48 is an activator of PDK1 with an AC50 of 8 μM.
    PS48
  • HY-172142
    PDK1-IN-4
    		Inhibitor
    PDK1-IN-4 (Compound R-29) is a PDK1 inhibitor. PDK1-IN-4 can be used for research of lung cancer.
    PDK1-IN-4
  • HY-N0047R
    Polyphyllin I (Standard)
    		Inhibitor
    Polyphyllin I (Standard) is the analytical standard of Polyphyllin I. This product is intended for research and analytical applications. 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 (Standard)
  • HY-11005
    BX-912
    		Inhibitor 99.13%
    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-124379
    TPCK
    		Inhibitor 98.55%
    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-10547
    OSU-03012
    		Inhibitor 98.88%
    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-14440
    MP7
    		Inhibitor 99.33%
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
    MP7
  • HY-W005629
    Leelamine
    		Inhibitor 98.36%
    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-121629
    PS210
    		Activator 98.30%
    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-13842
    BX517
    		Inhibitor ≥98.0%
    BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
    BX517
  • HY-114645
    PDK1-IN-RS2
    		Inhibitor 98.49%
    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-13856
    (R)-PS210
    		Inhibitor 98.09%
    (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-10515
    BX-320
    		Inhibitor 99.4%
    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-131962A
    PKD-IN-1 dihydrochloride
    		Inhibitor 99.58%
    PKD-IN-1 dihydrochloride (compound 32), an aminoethylamino-aryl (AEAA) compound, acts as PKD-1 inhibitor. PKD-IN-1 can be used for protein kinase D (PKD)-mediated diseases research.
    PKD-IN-1 dihydrochloride
  • HY-117809
    PDK1-IN-2
    		Inhibitor 98.90%
    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-13851
    PS47
    		98.83%
    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
Cat. No. Product Name / Synonyms Application Reactivity