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-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 99.78%
    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-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-15967
    PS48
    		Activator 99.71%
    PS48 is an activator of PDK1 with an AC50 of 8 μM.
    PS48
  • HY-W998345
    SMART1
    		Inhibitor
    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-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-W070306
    PDK1-IN-1
    		Inhibitor 99.95%
    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-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-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-14440
    MP7
    		Inhibitor 99.67%
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
    MP7
  • 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 98.50%
    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-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
  • HY-156375
    PKM2 activator 6
    		Inhibitor
    PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM).
    PKM2 activator 6
Cat. No. Product Name / Synonyms Application Reactivity