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PI3K/Akt/mTOR

Items 1-50 of 381

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  1. A10003
    MK-2206 2HCl

    AKT Inhibitor

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.
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  2. A10028
    Acadesine (Aicar,NSC 105823)

    AMPK activator

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

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  3. A10057
    Aloe-emodin

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

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  4. A10088
    AS-605240

    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.
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  5. A10094
    AT7867

    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.
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  6. A10112
    AZD6482

    PI3K inhibitor

    AZD6482 is a PI3Kbeta inhibitor (IC50=0.021M) used in antithrombotic therapy.
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  7. A10114
    AZD8055

    mTOR Inhibitor

    AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM.
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  8. A10133
    BEZ235 (NVP-BEZ235, Dactolisib)

    PI3K/mTOR Inhibitor

    BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
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  9. A10172
    CAL-101 (GS-1101, Idelalisib)

    PI3K inhibitor

    CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells.
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  10. A10199
    CHIR-99021

    GSK-3 Inhibitor

    CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.
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  11. A10295
    Deforolimus (Ridaforolimus)

    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.

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  12. A10374
    Everolimus (RAD001)

    mTOR inhibitor

    Everolimus (RAD-001) is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an mTOR inhibitor.
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  13. A10389
    FK-506 (Tacrolimus)

    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.
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  14. A10421
    GDC-0941 (Pictilisib)

    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.
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  15. A10438
    GSK1059615

    mTOR/PI3K Inhibitor

    GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM).
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  16. A10453
    Honokiol

    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.
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  17. A10463
    IC-87114

    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).
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  18. A10471
    Indirubin

    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.
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  19. A10505
    KU-0063794

    mTOR Inhibitor

    KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively).
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  20. A10506
    KU-55933

    ATM inhibitor

    KU-55933 is an ATM inhibitor by suppressing cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt.
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  21. A10507
    KU-60019

    ATM Inhibitor

    KU-60019 is a potent and specific ATM inhibitor with IC50 of 6.3 nM.
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  22. A10547
    LY294002

    PI3K Inhibitor

    LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.
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  23. A10681
    OSU-03012

    PDK-1 inhibitor

    OSU-03012 is a novel celecoxib derivative, without cyclooxygenase-2 inhibitory activity, capable of inducing apoptosis in various cancer cells types.
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  24. A10693
    Palomid 529 (P529)

    AKT Inhibitor

    Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation.
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  25. A10709
    Perifosine (NSC-639966)

    Akt inhibitor

    Perifosine (also KRX-0401) acts as an Akt inhibitor and a PI3K inhibitor.
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  26. A10717
    Phenformin hydrochloride

    Phenformin hydrochloride is a hydrochloride salt of phenformin from the biguanide drug class that displays anti-diabetic activity.
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  27. A10726
    PI-103

    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.
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  28. A10727
    PIK-293

    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.
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  29. A10728
    PIK-294

    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.
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  30. A10729
    PIK-75 hydrochloride

    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.
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  31. A10730
    PIK-90

    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.
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  32. A10731
    PIK-93

    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.
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  33. A10746
    PP242 (Torkinib)

    mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
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  34. A10765
    Quercetin dihydrate (Sophoretin)

    MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
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  35. A10766
    Quercetin (Sophoretin)

    MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
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  36. A10782
    Rapamycin (Sirolimus)

    mTOR Inhibitors

    Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).
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  37. A10825
    SB 216763

    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).
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  38. A10900
    Desmethyl-VS-5584

    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.
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  39. A10906
    Temsirolimus (Torisel)

    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.
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  40. A10922
    TG100-115

    PI3K Inhibitor

    TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).
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  41. A10923
    TGX-221

    PI3K Inhibitor

    TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.
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  42. A10989
    WYE-354

    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.
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  43. A10995
    XL147 analogue

    PI3K Inhibitor

    XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity.
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  44. A10997
    XL765

    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.
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  45. A11014
    ZSTK474

    PI3K inhibitor

    ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms.
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  46. A11016
    BKM120 (NVP-BKM120, Buparlisib)

    PI3K Inhibitor?€?

    BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor.
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  47. A11023
    GDC-0980 (Apitolisib, RG7422)

    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.
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  48. A11024
    PF-04691502

    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.
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  49. A11030
    GSK690693

    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).
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  50. A11031
    CCT128930

    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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