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PDK1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

47

Inhibitors & Agonists

1

Screening Libraries

1

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1

Peptides

5

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1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0645
    Dicoumarol
    Maximum Cited Publications
    11 Publications Verification

    Dicumarol

    Quinone Reductase PDHK Cancer
    Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.
    Dicoumarol
  • HY-10514
    BX795
    Maximum Cited Publications
    38 Publications Verification

    PDK-1 IKK Autophagy Cancer
    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
  • HY-N0047
    Polyphyllin I
    5 Publications Verification

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    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
  • HY-11005
    BX-912
    5+ Cited Publications

    PDK-1 Apoptosis Cancer
    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 .
    BX-912
  • HY-14981
    GSK2334470
    10+ Cited Publications

    PDK-1 Cancer
    GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
    GSK2334470
  • HY-10547
    OSU-03012
    5+ Cited Publications

    AR-12; PDK1 inhibitor AR-12

    PDK-1 Autophagy Cancer
    OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM .
    OSU-03012
  • HY-12492
    VER-246608
    4 Publications Verification

    PDHK Cancer
    VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
    VER-246608
  • HY-N6769
    Radicicol
    4 Publications Verification

    Monorden

    HSP Bacterial Antibiotic Parasite Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
    Radicicol
  • HY-124379
    TPCK
    1 Publications Verification

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    Ser/Thr Protease HPV Apoptosis PDK-1 Infection Neurological Disease Inflammation/Immunology Cancer
    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 .
    TPCK
  • HY-14440
    MP7
    2 Publications Verification

    PDK1 inhibitor

    PDK-1 Cancer
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
    MP7
  • HY-15569

    CDK Cancer
    NU6102 is a potent CDK1 and CDK2 inhibitor with IC50s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. NU6102 shows selectivity for CDK1/CDK2 over CDK4 (IC50 of 1.6 μM), DYRK1A (IC50 of 0.9 μM), PDK1 (IC50 of 0.8 μM) and ROCKII (IC50 of 0.6 μM) .
    NU6102
  • HY-19564
    JX06
    5+ Cited Publications

    PDHK Apoptosis Cancer
    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity .
    JX06
  • HY-121744
    PS10
    5+ Cited Publications

    PDHK Inflammation/Immunology
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
    PS10
  • HY-121629

    PDK-1 Cancer
    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 .
    PS210
  • HY-13842
    BX517
    2 Publications Verification

    PDK-1 Cancer
    BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
    BX517
  • HY-114645

    PDK-1 Cancer
    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 .
    PDK1-IN-RS2
  • HY-149814

    PDHK HSP Cancer
    PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass .
    PDK-IN-1
  • HY-124652

    IKK Cancer
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR .
    TBK1/IKKε-IN-4
  • HY-W070306

    PDK-1 FGFR Wee1 MARK Neurological Disease Cancer
    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-10515

    PDK-1 Cancer
    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 .
    BX-320
  • HY-W998345

    PROTACs PDK-1 Akt Cancer
    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)) .
    SMART1
  • HY-151465

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
    HIF-1α-IN-4
  • HY-106263B

    PTEN PDK-1 MDM-2/p53 Apoptosis Akt Cancer
    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 .
    Tyroserleutide hydrochloride
  • HY-117809

    PDK-1 Cancer
    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 .
    PDK1-IN-2
  • HY-157299

    PDHK Cancer
    PDK-IN-3 (compound 1) is a potent pan inhibitor of PDK with IC50s of 109.3, 135.8, 458.7 nM and 8.67 μM against PDK 1-4, respectively. PDK-IN-3 also induces proliferation and apoptosis in A549 cells .
    PDK-IN-3
  • HY-16461

    (-)-Solenopsin A

    Akt Ribosomal S6 Kinase (RSK) PI3K PDK-1 FOXO Mitophagy Reactive Oxygen Species (ROS) Mitochondrial Metabolism Cardiovascular Disease
    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-151466

    HIF/HIF Prolyl-Hydroxylase Monoamine Oxidase Cancer
    HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .
    HIF-1α-IN-5
  • HY-149275

    Pyruvate Kinase PDK-1 Akt EGFR Apoptosis Cancer
    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-124060

    PDK-1 Cancer
    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
  • HY-129426

    Akt Cancer
    PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway .
    PDK1/Akt/Flt dual pathway inhibitor
  • HY-10547R

    AR-12 (Standard); PDK1 inhibitor AR-12 (Standard)

    Reference Standards PDK-1 Autophagy Cancer
    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-177913

    PDK-1 Cancer
    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-12482

    PI3K Apoptosis PDK-1 MEK Akt ERK Cancer
    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-172142

    PDK-1 Cancer
    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

    PDK-1 Cancer
    PDK1-IN-3 (Compound C) is a PDK1 inhibitor, with an IC50 of 34 nM .
    PDK1-IN-3
  • HY-117885

    PDK-1 Cancer
    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-N0645S

    Dicumarol-d8

    Isotope-Labeled Compounds PDHK Cancer
    Dicoumarol-d8 (Dicumarol-d8) is the deuterium labeled Dicoumarol. Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.
    Dicoumarol-d8
  • HY-N0047R

    Reference Standards JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    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-156109

    PDHK Mitochondrial Metabolism Cancer
    PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
    PDK-IN-2
  • HY-156375

    Pyruvate Kinase PDK-1 Cancer
    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-179501

    PDK-1 Reactive Oxygen Species (ROS) Apoptosis Oxidative Phosphorylation Cancer
    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-175770

    Isocitrate Dehydrogenase (IDH) PDK-1 Apoptosis Cancer
    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-119134

    Akt Cancer
    PX-316 is an Akt inhibitor. PX-316 can phosphorylate Akt, but does not inhibit the phosphorylation of PDK1 or PKC. PX-316 uniquely increases the expression of a group of mitochondrial-related genes. PX-316 can be used for the study of colon cancer and breast cancer .
    PX-316
  • HY-N17990

    PDK-1 Akt GSK-3 Reactive Oxygen Species (ROS) Neurological Disease
    Sexangularetin 3-sophoroside is a PDK1 and Akt phosphorylation activator with neuroprotective properties. Sexangularetin 3-sophoroside restores phosphorylated GSK-3β protein levels. Sexangularetin 3-sophoroside acts as a ROS inhibitor and regulates mRNA expression of superoxide dismutase 1 and catalase. Sexangularetin 3-sophoroside can be used for the research of Parkinson’s disease .
    Sexangularetin 3-sophoroside
  • HY-10514R

    Reference Standards PDK-1 IKK Autophagy Cancer
    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)
  • HY-181670

    Androgen Receptor c-Myc Akt mTOR ERK PDK-1 PI3K Apoptosis Metabolic Disease Cancer
    WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer .
    WH23
  • HY-183583

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].
    HIF-2α-IN-18

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