PI3K/Akt/mTOR

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  1. CMK

    RSK2 kinase inhibitor

    CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.
  2. mTOR inhibitor

    GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases.
  3. PI3Kα/δ inhibitor

    Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
  4. Akt inhibitor

    Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM).
  5. PI3K/PDK-1 Inhibitor

    NVP-BAG956 acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor, displaying much reduced potency against VEGFR1 (IC50 = 2.56 uM) and little or no activity toward a panel of 15 other kinases (IC50 >10 uM).
  6. PDK1 inhibitor

    PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent.
  7. mTORC1/2 inhibitor

    QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.
  8. DNA-PK inhibitor

    Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM).
  9. GSK-3 Inhibitor

    TDZD-8 protects the brain against I/R injury by inhibiting GSK-3beta activity
  10. mTOR inhibitor

    Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier.
  11. PI3K inhibitor

    TG 100713 is an inhibitor of PI3-kinase that inhibits endothelial cell proliferation.
  12. Akt inhibitor

    SC 66 is an allosteric inhibitor of Akt that facilitates both ubiquitination and deactivation of Akt. It exhibits anticancer activity in vitro and in vivo.
  13. HDACs/mTOR Inhibitor 1

    HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies.
  14. PTEN inhibitor

    SF1670 is a selective PTEN inhibitor (IC50=2 uM). As PTEN-mTOR pathway is critical for controlling the regenerative capacity of corticospinal neurons, PTEN deletion or its inhibitor enhances the regenerative ability of adult corticospinal neurons. Pretreatment with SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model.
  15. AKT inhibitor

    SR-13668 is an Akt inhibitor, is also an orally bioavailable indole-3-carbinol (I3C) analogue inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic and antiangiogenic activities.
  16. PI3Kδ inhibitor

    Parsaclisib is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
  17. PI4K inhibitor

    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 ?M).
  18. AKT/PKB inhibitor

    10-DEBC HCl is a selective inhibitor of Akt/PKB. It inhibits IGF-1-stimulated phosphorylation and activation of Akt (complete inhibition at 2.5 μM), suppressing downstream activation of mTOR, p70 S6 kinase and S6 ribosomal protein.
  19. PI3Kα inhibitor

    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
  20. PI3K inhibitor

    GNE-317 is a potent PI3K inhibitor that can cross the Blood?? brain barrier; shows potent suppression of the PI3K pathway in the brain of mice with intact BBB.
  21. PI3Kδ inhibitor

    PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
  22. PI3K/mTOR inhibitor

    GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
  23. Broad-Spectrum Kinase Inhibitor

    CTX-0294885 is a novel broad-spectrum kinase inhibitor. CTx-0294885 exhibits inhibitory activity against a broad range of kinases in vitro.
  24. ATR/CDK inhibitor

    NU6027 is a potent inhibitor of cellular ATR activity (IC(50)=6.7 μM) and enhanced hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
  25. PI3K/Akt inhibitor

    Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa
  26. PI3K inhibitor

    (Rac)-AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.

  27. GSK-3β inhibitor

    IM-12 is a cell-permeable indolylmaleimide that acts as a Glycogen synthase kinase 3β (GSK-3β) inhibitor, activating downstream components of canonical Wnt signaling.
  28. GSK-3β inhibitor

    1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.
  29. NUAK kinase inhibitor

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2
  30. pan-RSK inhibitor

    LJH685 is a potent , specific and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50 of 4 to 13 nM.
  31. RSK inhibitor

    LJI308 is a new and potent pan-RSK inhibitor, with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.
  32. PI3K inhibitor

    Panulisib is a potent and selective imidazoquinoline based PI3K inhibitor with potential anticancer activity.
  33. Dual Pan PI3k/mTOR inhibitor

    GNE-493 is potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitor with potential anticancer activity.
  34. PI3Kδ Inhibitor

    Acalisib is an inhibitor of the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities.
  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. BIO

    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. mTOR/DNA-PK inhibitor

    CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
  43. Akt inhibitor

    Akt inhibitor GSK2141795 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis.
  44. ACL inhibitor and AMPK activator

    ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
  45. ATM Inhibitor

    Mirin prevents ATM activation in response to double strand breaks (IC50 = 12 uM) and induces G2 cell cycle arrest.
  46. Autophagy Inhibitor

    Vps34-PIK-III (PIK-III) is a selective inhibitor of VPS34 enzymatic activity.

  47. Vps34 Inhibitor

    Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
  48. PI3Kδ inhibitor

    AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
  49. Akt Inhibitor

    TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
  50. PI3K inhibitor

    PQR309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

Items 451-500 of 860

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