1. PI3K/Akt/mTOR
  2. PDK-1

PDK-1

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.

PDK-1 Related Products (21):

Cat. No. Product Name Effect Purity
  • HY-14981
    GSK2334470 Inhibitor 99.78%
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
  • HY-10514
    BX795 Inhibitor 99.17%
    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[1][2][3][4].
  • 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[1].
  • HY-N0047
    Polyphyllin I Inhibitor
    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[1][2][3].
  • HY-14440
    MP7 Inhibitor 99.67%
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
  • HY-W070306
    PDK1-IN-1 Inhibitor
    PDK1-IN-1 (Compound 2-11) is a PDK1 inhibitor, and can be used for research of myeloproliferative disorders or cancer[1].
  • 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[1].
  • 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)[1].
  • HY-P5450
    PDKtide
    PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)
  • 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[1][3].
  • HY-15967
    PS48 Activator 99.78%
    PS48 is an activator of PDK1 with an AC50 of 8 μM.
  • 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[1].
  • 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[1][2].
  • HY-13842
    BX517 Inhibitor
    BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
  • HY-13856
    (R)-PS210 Inhibitor 98.20%
    (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[1].
  • HY-10515
    BX-320 Inhibitor
    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[1].
  • 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[1].
  • HY-135773
    CRTh2 antagonist 3 Activator
    CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. 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[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[1][2].
  • 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[1].