PI3K/Akt/mTOR

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  1. GSK-3 inhibitor

    GSK-3 inhibitor 1 is an inhibitor of GSK-3.
  2. multi-kinase inhibitor

    Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle.
  3. multi-kinase inhibitor

    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle.
  4. AMPK allosteric activator

    ZLN024 is an AMPK allosteric activator.
  5. Akt inhibitor

    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  6. PI3Kδ inhibitor

    Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
  7. PDK inhibitor

    VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
  8. GSK-3β inhibitor

    9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM.
  9. Akt inhibitor

    API-1 (NSC 177223) is a potent inhibitor of Akt that induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis.
  10. PDK1 inhibitor

    PS210 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site.
  11. GSK-3 inhibitor

    GSK3 Inhibitor XIII (GSK3i XIII) is an ATP-binding site inhibitor of GSK-3.
  12. ATR inhibitor

    Gartisertib (VX-803, ATR inhibitor 2) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM.

  13. MELK inhibitor

    OTSSP167 (hydrochloride) is a highly potent MELK inhibitor with IC50 value of 0.41 nM.
  14. lysosomal exocytosis inhibitor

    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor.
  15. pan-PI3K inhibitor

    GNE-490 is a highly selective pan-PI3K inhibitor that demonstrates selectivity over mTOR.
  16. mitochondria-targeted antioxidant

    Demethyleneberberine is a natural mitochondria-targeted antioxidant.
  17. PDK inhibitor

    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively.
  18. bitter taste receptor TAS2R1 agonist

    Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α.
  19. NF-κB inhibitor

    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass.
  20. ChoKα inhibitor

    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1.
  21. Gβγ subunit signalling inhibitor

    Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent.
  22. Syk/PI3K inhibitor

    SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
  23. PTEN inhibitor

    BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity.
  24. flavonoid

    Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
  25. AMPK activator

    IM156 (HL156A), a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation.
  26. RSK inhibitor

    S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K).
  27. AMPK activator

    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
  28. mTOR activator

    3BDO is a new mTOR activator which can also inhibit autophagy.
  29. PI3Kδ inhibitor

    Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
  30. Akt inhibitor

    Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
  31. PI3Kδ inhibitor

    Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
  32. anti-tumor agent

    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory.
  33. monounsaturated fatty acid

    Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia .
  34. anti-inflammatory agent

    Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities.
  35. AMPK activator

    PF-06679142 is a potent AMPK activator. PF-06679142 exhibited robust activation of AMPK in rat kidneys as well as desirable oral absorption, low plasma clearance, and negligible renal clearance in preclinical species.
  36. NV-5138 is an active small-molecule drug for the treatment of major depressive disorder (MDD).
  37. PI3Kδ inhibitor

    PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
  38. PI3Kγ inhibitor

    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  39. dual pan-PI3K/mTOR inhibitor

    PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
  40. AMPK activator

    O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK.
  41. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
  42. ATR inhibitor

    ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 ?μ.
  43. ATM inhibitor

    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM.
  44. PI4KIIIβ inhibitor

    UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases.
  45. PI3Kδ/PI3Kγ inhibitor

    Tenalisib R Enantiomer is an R enantiomer of Tenalisib.
  46. GSK-3 inhibitor

    A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β.
  47. PI3Kδ inhibitor

    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM.
  48. DNA-PK inhibitor

    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
  49. mTOR inhibitor

    mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
  50. DNA-PK inhibitor

    AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumor activity.

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