PI3K/Akt/mTOR

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  1. S6 kinase inhibitor

    PF 4708671 is a highly specific inhibitor of p70 ribosomal S6 kinase (S6K1) that inhibits S6K1-mediated phosphorylation of S6 protein in response to IGF-1 , while having no effect on highly related RSK and MSK kinases.
  2. mTOR inhibitor

    INK 128 is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
  3. AKT inhibitor

    AKT inhibitor VIII is a cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 μM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays).
  4. Akt phosphorylation activator

    SC79 is an AKT activator. SC79 binds to the plecktrin homology (PH) domain of Akt that mimics the binding of PtdIns(3,4,5)P3 to induce a conformational change in Akt that enhances phosphorylation and activation.
  5. Akt inhibitor

    Perifosine (also KRX-0401) acts as an Akt inhibitor and a PI3K inhibitor.
  6. PI3K/HDAC inhibitor

    CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.
  7. Akt inhibitor

    A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.
  8. DNA-PK inhibitor

    NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.
  9. DNA-PK inhibitor

    NU7026 is a novel DNA-dependent protein kinase inhibitor that potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia.
  10. Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
  11. Deguelin is a natural product that displays profound antiproliferative activity.
  12. GSK-3 inhibitor

    AR-A 014418 is a selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.
  13. AMPK activator

    EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.
  14. mTOR inhibitor

    Torin1 is a potent inhibitor of mTOR with IC50 of 2-10 nM.
  15. mTOR inhibitor

    Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).
  16. PI3K Inhibitor

    PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.
  17. PI3K Inhibitor

    LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.
  18. ATM Inhibitor

    KU-60019 is a potent and specific ATM inhibitor with IC50 of 6.3 nM.
  19. ATR inhibitor

    ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
  20. PI4K inhibitor

    PIK 93 selectively inhibits the type III PI 4-kinase enzyme, and small interfering RNA-mediated down-regulation of the individual PI 4-kinase enzymes.
  21. BMP inhibitor

    Dorsomorphin, also known as BML-275, is a selective small molecule inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.
  22. mTOR Inhibitor

    WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of PI3K α (IC50 = 1026 nM) and other kinases.
  23. AMPK activator

    GSK621 is a potent and selective AMPK agonist.
  24. PDK-1 inhibitor

    BX-795 is a potent PDK1 inhibitor that blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis.
  25. FMK

    RSK inhibitor

    FMK is potent, highly specific and irreversible inhibitor of p90 ribosomal protein S6 kinase RSK1 and RSK2; Fmk binds in the CTKD ATP-binding site and inhibits RSK autophosphorylation at Ser386. Fmk induces significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells.
  26. PI3Kα/PI3Kδ inhibitor

    AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50 of 5.7 nM and 6.2 nM, with selectivity against PI3Kβ (IC50 431 nM) and PI3Kγ (IC50 90 nM).
  27. mTOR/PI3K Inhibitor

    GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM).
  28. AMP-activated protein kinase (AMPK) activator

    Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose.
  29. ATR inhibitor

    Berzosertib (VE-822) is an potent ATR inhibitor.

     
  30. ATR inhibitor

    BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
  31. ATR inhibitor

    AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.
  32. mTOR Inhibitor

    AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM.
  33. p70S6K inhibitor

    LY-2584702 is an orally available inhibitor of p70S6K signaling; inhibits p70S6K and prevents phosphorylation of the S6 subunit of ribosomes.
  34. mTOR/PI3K Inhibitor

    GDC-0980 (RG7422) is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms, respectively.
  35. ATM inhibitor

    KU-55933 is an ATM inhibitor by suppressing cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt.
  36. PI3K inhibitor

    AZD6482 is a PI3Kbeta inhibitor (IC50=0.021M) used in antithrombotic therapy.
  37. PI3K Inhibitor

    BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor.
  38. PI3K inhibitor

    CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells.
  39. PI3K Inhibitor

    TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.
  40. PI3K inhibitor

    CZC24832 is a selective inhibitor of PI 3-Kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay).
  41. AKT inhibitor

    GSK690693 is a novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor (IC50 values are 2, 13 and 9 nM of Akt1, 2 and 3 respectively).
  42. PI3K inhibitor

    GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively.
  43. PI3K/mTOR Inhibitor

    BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
  44. mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
  45. PI3K Inhibitor

    YM201636 is a cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM).
  46. AKT inhibitor

    Capivasertib (AZD5363) is a potent inhibitor of AKT with pharmacodynamic activity in vivo, has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent.

  47. Aloe emodin is a anthraquinone present in aloe latex, an exudate from the aloe plant. It has a strong stimulant-laxative action.

  48. mTOR inhibitor

    Everolimus (RAD-001) is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an mTOR inhibitor.
  49. Autophagy/PI3K Inhibitor

    3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
  50. AMPK activator

    A-769662 is a new activator of AMP-activated protein kinase (AMPK).

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