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-P5450
    PDKtide
    PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)
    PDKtide
  • HY-13844
    PDK1-IN-3
    		Inhibitor
    PDK1-IN-3 (Compound C) is a PDK1 inhibitor, with an IC50 of 34 nM.
    PDK1-IN-3
  • HY-146977
    LDHA/PDKs-IN-1
    		Inhibitor
    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-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.
    CRTh2 antagonist 3
  • HY-146978
    LDHA/PDKs-IN-2
    		Inhibitor
    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-149275
    PKM2/PDK1-IN-1
    		Inhibitor
    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-117885
    PF-5177624
    		Inhibitor
    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-124060
    PS423
    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
Cat. No. Product Name / Synonyms Application Reactivity