PI3K/Akt/mTOR

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  1. AKT Inhibitor

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.
  2. AMPK activator

    Acadesine is a selective activator of AMPK in both hepatocytes and adipocytes.

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

  4. PI3K Inhibitor

    AS-605240 is an orally active inhibitor of PI3-kinase γ that inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.
  5. AKT inhibitor

    AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A.
  6. PI3K inhibitor

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

    AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM.
  8. PI3K/mTOR Inhibitor

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

    CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells.
  10. GSK-3 Inhibitor

    CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.
  11. mTOR Inhibitor

    Deforolimus (Ridaforolimus) is an investigational targeted and small-molecule inhibitor of the protein mTOR. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.

  12. mTOR inhibitor

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

    FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.
  14. 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.
  15. mTOR/PI3K Inhibitor

    GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM).
  16. Antiangiogenic and Antitumor Agent

    Honokiol is a lignan present in the cones, bark, and leaves of Magnolia grandiflora that has shown pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines.
  17. PI3K Inhibitor

    IC-87114 was the first isoform-selective PI3K inhibitor :p110M-NM-4(IC50 = 0.13 M-BM-5M) vs. p110M-NM-1(IC50 = 200 M-BM-5M), p110M-NM-2(IC50 = 16 M-BM-5M) and p110M-NM-3(IC50 = 61 M-BM-5M).
  18. CDK & GSK-3β inhibitor

    Indirubin, the active constituent of a Chinese antileukaemia medicine, is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.
  19. mTOR Inhibitor

    KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively).
  20. ATM inhibitor

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

    KU-60019 is a potent and specific ATM inhibitor with IC50 of 6.3 nM.
  22. PI3K Inhibitor

    LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.
  23. PDK-1 inhibitor

    OSU-03012 is a novel celecoxib derivative, without cyclooxygenase-2 inhibitory activity, capable of inducing apoptosis in various cancer cells types.
  24. AKT Inhibitor

    Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation.
  25. Akt inhibitor

    Perifosine (also KRX-0401) acts as an Akt inhibitor and a PI3K inhibitor.
  26. Phenformin hydrochloride is a hydrochloride salt of phenformin from the biguanide drug class that displays anti-diabetic activity.
  27. 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.
  28. PI3K inhibitor

    PIK-293 is a PI3-K inhibitor. PIK-293 inhibits the p110α, p110β, p110δ. PIK-293 is the parent compound of PIK-294.
  29. PI3K inhibitor

    PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110δ-selective inhibitors that has been reported.
  30. PI3K Inhibitor

    PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 μM and 1.3 μM, respectively.
  31. PI3K Inhibitor

    PIK-90 is a synthetic phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity.
  32. 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.
  33. mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
  34. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  35. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  36. mTOR Inhibitors

    Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).
  37. GSK-3 inhibitor

    SB 216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).
  38. PI3K/mTOR inhibitor

    Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
  39. mTOR inhibitor

    Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells.
  40. PI3K Inhibitor

    TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).
  41. PI3K Inhibitor

    TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.
  42. 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.
  43. PI3K Inhibitor

    XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity.
  44. PI3K inhibitor

    XL765 is a PI3K/mTOR dual kinase inhibitor and it is more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.
  45. PI3K inhibitor

    ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms.
  46. PI3K Inhibitor?€?

    BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor.
  47. 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.
  48. PI3K/mTOR Inhibitor

    PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.
  49. 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).
  50. AKT Inhibitor

    CCT128930 is an ATP-competitive AKT inhibitor that is a potent, advanced lead pyrrolopyrimidine compound exhibiting selectivity for AKT over PKA, achieved by targeting a single amino acid difference.

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