PI3K/Akt/mTOR

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  1. 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.
  2. 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.
  3. ChoKα inhibitor

    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1.
  4. 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.
  5. 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.
  6. PTEN inhibitor

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

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

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

    S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K).
  10. 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.
  11. mTOR activator

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

    Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
  13. 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.
  14. 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].
  15. 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.
  16. 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 .
  17. 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.
  18. 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.
  19. NV-5138 is an active small-molecule drug for the treatment of major depressive disorder (MDD).
  20. HDR inhibitor

    YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
  21. p110β inhibitor

    Rac)-AZD 6482 ((Rac)-KIN-193) is a less active racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
  22. PI3K β/δ inhibitor

    PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively.
  23. PI3Kδ inhibitor

    LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
  24. CaM-KK inhibitor

    STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.
  25. SHIP-2 inhibitor

    AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5?? phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.
  26. ILK inhibitor

    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain).
  27. AKT1/AKT2 inhibitor

    3CAI is a potent and specific AKT1 and AKT2 inhibitor.
  28. ATM inhibitor

    KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM.
  29. PI3Kδ inhibitor

    CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
  30. AKT inhibitor

    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  31. GSK2110183 analog 1 is the structural analogue of GSK2110183.
  32. ATP-competitive AKT inhibitor

    Solenopsin is an ATP-competitive AKT inhibitor with IC50 value of 10 μM .
  33. PI3K/Akt activator

    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells.
  34. PI3KC3 isoform Vps34 inhibitor

    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PI3KC3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM).
  35. (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Nedisertib, with an IC50 in the range of 7-30 nM for DNA-PK.
  36. DNA-PK inhibitor

    (Rac)-Nedisertib ((Rac)-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM.
  37. mTOR inhibitor

    42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor.
  38. p70S6K inhibitor

    LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  39. GSK-3α/β inhibitor

    CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
  40. GSK-3α/β inhibitor

    CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM.
  41. PI3Kδ inhibitor

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

    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  43. 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.
  44. AMPK activator

    O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK.
  45. 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.
  46. ATR inhibitor

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

    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM.
  48. 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.
  49. PI3Kδ/PI3Kγ inhibitor

    Tenalisib R Enantiomer is an R enantiomer of Tenalisib.
  50. 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.

Items 701-750 of 1059

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