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

PDK-1 Inhibitor

PDK-1 Inhibitors (24):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-14981
    GSK2334470
    		Inhibitor 99.79%
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
  • 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.
  • 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.
  • HY-W998345
    SMART1
    		Inhibitor 99.31%
    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)) .
  • HY-13844
    PDK1-IN-3
    		Inhibitor
    PDK1-IN-3 (Compound C) is a PDK1 inhibitor, with an IC50 of 34 nM.
  • 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.
  • 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.
  • 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.
  • HY-14440
    MP7
    		Inhibitor 99.33%
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
  • 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 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.
  • 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.
  • 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.
  • 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.
  • HY-106263B
    Tyroserleutide hydrochloride
    		Inhibitor 99.47%
    Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis.
  • 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).
  • 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.
  • 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.
  • 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.