PI3K/Akt/mTOR

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  1. dual PI3K and BCR-ABL inhibitor

    ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM.
  2. PI4KIIIβ inhibitor

    PI4KIIIbeta-IN-10 is the most potent PI4KIIIbeta inhibitor currently reported, with very minor off-target inhibition of PI4KIIIbeta related lipid kinases (IC50 = 3.6 nM).
  3. PI4KIIIβ inhibitor

    PI4KIIIbeta-IN-9 is a potent PI4KIIIbeta inhibitor (IC50 of 7 nM) and is >140-fold selective over PI3Kgamma and >20-fold selective over PI3Kδ, and shows no inhibition of vps34 at concentrations up to 20 uM.
  4. PI3K α/δ inhibitor

    ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing.
  5. PI3K inhibitor

    GDC-0084 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
  6. PI3K inhibitor

    NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM.
  7. PI3Kα inhibitor

    PI3Kα inhibitor 1 is a PI3Kα inhibitor extracted from patent US/20120088764A1, compound 243, has an IC50 < 0.1 uM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 uM ??? IC50 ??? 1 uM) .
  8. PI3Kγ inhibitor

    PI3Kγ inhibitor 1 is a potent PI3Kγ inhibitor.
  9. PI3K/mTOR dual inhibitor

    SAR245409 is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity.
  10. PI3Kδ inhibitor

    TGR-1202 is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.
  11. PI3Kδ inhibitor

    TGR-1202 hydrochloride is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.
  12. GSK-3β inhibitor

    Indirubin-3'-monoxime is a powerful inhibitor of GSK-3β with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM).
  13. NUAK1 inhibitor

    HTH-01-015 is a potent and selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.
  14. AKT 1/2 inhibitor

    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.
  15. AKT inhibitor

    ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).
  16. PI3Kγ Inhibitor

    IPI-549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM.
  17. 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).
  18. Akt inhibitor

    Afuresertib is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.
  19. ATM inhibitor

    AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.
  20. mTOR inhibitor

    CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
  21. PI3Kδ inhibitor

    GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM). GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases.
  22. S6K inhibitor

    Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle.
  23. PI3K inhibitor

    Leniolisib(CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.
  24. PI3K inhibitor

    Seletalisib is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold).
  25. ATM inhibitor

    AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
  26. dual PI3Kδ/γ inhibitor

    Tenalisib, also known as RP6530, is a potent and selective dual PI3Kδ/γ inhibitor that inhibited growth of B-cell lymphoma cell lines with a concomitant reduction in the downstream biomarker, pAKT.
  27. selective p110δ inhibitor

    IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5??1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
  28. ATM inhibitor

    AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
  29. ATM inhibitor

    AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
  30. SUMO inhibitor

    2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
  31. 4EBP1 inhibitor

    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  32. PI3Kβ inhibitor

    SAR260301 is potent and selective Class I phosphatidylinositol-3-kinase (PI3K)β specific inhibitor with an IC50 of 52 nM for this isoform.
  33. Vps34 inhibitor

    Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively.
  34. PI4K inhibitor

    BQR-695, also known as NVP-BQR695, is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
  35. DNA-PK inhibitor

    Nedisertib, also known as M-3814, MSC2490484A, is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities.
  36. PI4K inhibitor

    KDU691 is a plasmodium PI4K inhibitor (IC50 values of 0.18 μM and 0.061 μM against hypnozoite forms and liver schizontsm, respectively).
  37. GSK3 inhibitor

    BIO is a cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β with IC50 value of 5 nM.
  38. EGFR/PI3K dual inhibitor

    MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.
  39. P110δ inhibitor

    P110δ-IN-1 is a potent and selective inhibitor of P110δ extracted from patent WO 2014055647 A1, with an IC50 of 8.4 nM.
  40. Pin1 inhibitor

    TAB29 is a potent inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) with an IC50 of 874?nM, possesses therapeutic potential for human cancers.
  41. PDK inhibitor

    KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.
  42. dual PDE7/GSK-3 inhibitor

    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  43. prolyl isomerase PIN1 inhibitor

    KPT-6566, a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 of 640?nM and a Ki of 625.2 nM for PIN1 PPIase domain. Anti-cancer activity.
  44. GSK-3β inhibitor

    GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.
  45. PI3Kγ inhibitor

    PI3Kγ inhibitor 3 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.
  46. dual pan-PI3K/mTORC1/2 inhibitor

    PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.
  47. mTORC1/mTORC2 inhibitor

    FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.
  48. PI4KB inhibitor

    T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
  49. PI3Kδ inhibitor

    PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
  50. PI4K inhibitor

    UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.

Items 201-250 of 331

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