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

PDK-1

PDK-1 (phosphoinositide dependent protein kinase-1) is a protein which in humans is encoded by the PDK1 gene. It is implicated in the development and progression of melanomas. PDK-1 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 PDK-1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling. More recent data indicate that alteration of PDK-1 is a critical component of oncogenic PI3K signalling in breast cancer, suggesting that inhibition of PDK-1 can inhibit breast cancer progression. PDK-1 has an essential role in regulating cell migration especially in the context of PDK-1 deficiency. PDK-1 is a valid therapeutic target and suggests that PDK-1 inhibitors may be useful to prevent cancer progression and abnormal tissue dissemination.

PDK-1 Related Products (10):

Cat. No. Product Name Effect Purity
  • HY-10514
    BX795 Inhibitor 99.33%
    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 IKKɛ, 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.
  • HY-14981
    GSK2334470 Inhibitor 99.91%
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
  • HY-14440
    MP7 Inhibitor 99.83%
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
  • HY-11005
    BX-912 Inhibitor 99.53%
    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.
  • HY-13842
    BX517 Inhibitor >98.0%
    BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
  • HY-114645
    PDK1-IN-RS2 Inhibitor
    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.
  • HY-121629
    PS210 Activator
    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.
  • HY-13856
    (R)-PS210 Inhibitor
    (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.
  • HY-N0047
    Polyphyllin I Inhibitor >98.0%
    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.
  • HY-135773
    CRTh2 antagonist 3 Activator
    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.
Isoform Specific Products

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