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-W070306
    PDK1-IN-1
    		Inhibitor 99.95%
    PDK1-IN-1 (Compound 2-11) is a PDK1 inhibitor. PDK1-IN-1 is also useful as inhibitor of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. PDK1-IN-1 selectively inhibits microtubule affinity regulating kinase (MARK). PDK1-IN-1 can be used for researches of myeloproliferative disorders, cancer and Alzheimer's disease.
    PDK1-IN-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).
    PKM2 activator 6
  • 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-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-177913
    OSU-02067
    		Inhibitor
    OSU-02067 is a selective 3-phosphoinositide-dependent protein kinase-1 (PDK-1) inhibitor (IC50=9 μM). OSU-02067 is promising for research of solid tumors (e.g., prostate, breast, colorectal cancers).
    OSU-02067
  • 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-16461
    Solenopsin
    		Inhibitor
    Solenopsin ((-)-Solenopsin A) is an ATP-competitive and selective Akt-1 inhibitor with an IC50 of 5-10 μM, and also acts as an RSK1 inhibitor. Solenopsin inhibits the activities of PDK1 in lipid rafts, downregulates PI3K, blocks PI3K-dependent generation of 3-phosphoinositides, and suppresses the phosphorylation of FOXO1a. Solenopsin induces Mitophagy and ROS production, reduces mitochondrial oxygen consumption, and exhibits antiproliferative and antiangiogenic activities. Solenopsin can be used in research related to hyperproliferative skin diseases and malignant diseases.
    Solenopsin
  • HY-179501
    PDK1-IN-5
    		Inhibitor
    PDK1-IN-5 is a selective PDK1 inhibitor. PDK1-IN-5 activaties PDH by diminishing phosphorylation level via PDK1 inhibition. PDK1-IN-5 effectively reverses the Warburg effect and shifts cellular energy metabolism from glycolysis toward oxidative phosphorylation by increased acetyl-CoA, reduced lactate, elevated mitochondrial ROS, and subsequent induction of apoptosis. PDK1-IN-5 robustly inhibits tumor growth in vivo without inducing systemic toxicity. PDK1-IN-5 can be used for lung adenocarcinoma, human non-small cell lung adenocarcinoma and gastric colorectal.
    PDK1-IN-5
  • HY-12482
    X-370
    		Inhibitor
    X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).
    X-370
  • 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-10547R
    OSU-03012 (Standard)
    		Inhibitor
    OSU-03012 (Standard) is the analytical standard of OSU-03012 (HY-10547). This product is intended for research and analytical applications. OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM.
    OSU-03012 (Standard)
  • 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-175770
    mIDH1-IN-2
    		Inhibitor
    mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma.
    mIDH1-IN-2
  • HY-10514R
    BX795 (Standard)
    		Inhibitor
    BX795 (Standard) is the analytical standard of BX795 (HY-10514). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity