LY294002 / Eli Lilly 
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  • ||||||||||  LY294002 / Eli Lilly
    The cysteine-rich protein 61 (Cyr61) contributes to tumor proliferation and invasion via HGF-mediated NF-kB signaling pathway in human hepatocellular carcinoma (Hall Bordeaux) -  Jan 31, 2023 - Abstract #ESMOTAT2023ESMO_TAT_186;    
    To identify associated pathway of HGF-induced Cyr61 about IL-8, NF-?B expression, the cells were treated with PI3K (Phosphoinositide 3-kinase) inhibitor (LY294002) and then analyzed by Western blotting...HGF-mediated cell proliferation and invasion were decreased in Cyr61 knock down cell. Conclusions These results suggest that Cry61 plays an important role in cell proliferation and metastasis in hepatocellular carcinoma, and Cry61 may be a novel target for the prevention of progression and treatment of hepatocellular carcinoma.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  rhMYDGF Alleviates I/R-induced Kidney Injury by Inhibiting Inflammation and Apoptosis via the Akt Pathway. (Pubmed Central) -  Jan 27, 2023   
    Conclusions These results suggest that Cry61 plays an important role in cell proliferation and metastasis in hepatocellular carcinoma, and Cry61 may be a novel target for the prevention of progression and treatment of hepatocellular carcinoma. rhMYDGF protects kidney from I/R injury by attenuating oxidative stress, inflammation, and apoptosis through the activation of the Akt pathway.
  • ||||||||||  LY294002 / Eli Lilly
    Preclinical, Journal:  GPR30 Alleviates Pressure Overload-Induced Myocardial Hypertrophy in Ovariectomized Mice by Regulating Autophagy. (Pubmed Central) -  Jan 22, 2023   
    In summary, our results demonstrate that G1 can attenuate cardiac hypertrophy and fibrosis and improve the cardiac function of mice in the OVX + TAC group through AKT/mTOR mediated inhibition of autophagy. Thus, this study demonstrates a potential option for the drug treatment of pressure overload-induced cardiac hypertrophy in postmenopausal women.
  • ||||||||||  Journal:  Defining the role of mTOR pathway in the regulation of stem cells of glioblastoma. (Pubmed Central) -  Jan 20, 2023   
    Here we explored the role of the mTOR pathway in the regulation of stem cells of GBM by treating them with inhibitors of canonical PI3K/AKT/mTOR pathways such as rapamycin (mTORC1 inhibitor), PP242 (ATP binding mTORC1/2 inhibitor), LY294002 (PI3K inhibitor), and MAPK inhibitor, U0126...Treatment with novel small molecule inhibitors of mTORC1/2 demonstrated that Torin1 and Torin2 suppressed the proliferation of GBM CSC, while XL388 was less effective...Torin2 was able to eradicate tumor cells. In conclusion, Torin2 effectively targeted CSCs of GBM by halting self-renewal and inhibiting cell proliferation, underscoring the use of Torin2 in the treatment of GBM.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  SRC-3/TRAF4 facilitates ovarian cancer development by activating the PI3K/AKT signaling pathway. (Pubmed Central) -  Jan 11, 2023   
    Taken together, our study demonstrated that RPL22L1 is a key gene in PCa progression and promotes PCa cell proliferation and invasion via PI3K/Akt/mTOR pathway, thus potentially providing a new target for PCa therapy. Our study demonstrated that SRC-3/TRAF4 promotes ovarian cancer cell growth, migration, invasion, and stemness by activating the PI3K/AKT pathway.
  • ||||||||||  LY294002 / Eli Lilly, AG1478 / IDT Australia
    Journal:  Cryptosporidium parvum maintains intracellular survival by activating the host cellular EGFR-PI3K/Akt signaling pathway. (Pubmed Central) -  Jan 10, 2023   
    The EGFR inhibitor AG1478 decreased EGFR and Akt phosphorylation, and the PI3K inhibitor LY294002 impaired Akt phosphorylation induced by C. parvum in HCT-8 cells...Intracellular parasite proliferation was decreased when treated with autophagy inducer rapamycin, whereas autophagy inhibitor 3-MA, E64d+pep A, siBeclin1 or siATG7 increased intracellular parasites...In summary, C. parvum could maintain intracellular survival by inhibiting autophagy via EGFR-PI3K/Akt pathway. These results revealed a new mechanism for the interaction of C. parvum with host cells.
  • ||||||||||  LY294002 / Eli Lilly
    Embryonic signal regulates the porcine trophoblast cell functions () -  Jan 8, 2023 - Abstract #Fertility2023Fertility_388;    
    This biphasic manner of E2 release by embryos affects the endometrium and prolongs progesterone production by the corpus luteum...Confluent trophoblast cells (50-60%) were treated with vehicle or 100 nM E2, with/without 1 M of estrogen receptor antagonist (ICI182780) and 25 M PD098059, 25 M LY294002 (proliferation and adhesion assays), 2.5 M Akt1/2 kinase inhibitor or 50 nM rapamycin (only in proliferation assay) for 24 h. Cell proliferation and adhesion were assessed using colorimetric methods...Co-treatment with ICI182780 and selected inhibitors diminished stimulating effect of E2 in both processes. Results of the present study indicate that E2 secreted by the conceptuses likely controls in an autocrine manner the processes crucial for the proper development of embryos and placenta.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Transcriptional regulation of Notch1 by nuclear factor-κB during T cell activation. (Pubmed Central) -  Jan 3, 2023   
    Both the surface expression and mRNA transcription of Notch1 were significantly higher in activated CD4 T cells, but the inhibition of phosphatidylinositol 3-kinase (PI3K) by LY294002 or deletion of the Pdk1 gene impaired this upregulation of Notch1...In addition, inhibition of NF-κB by SN50 impaired upregulation of Notch1 surface protein and mRNA in activated CD4 T cells. Thus, we provide evidence that Notch1 transcription in activated CD4 T cells is upregulated via the PI3K-PDK1-NF-κB signaling pathway.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  The Neuroprotective Effects of Arecae Pericarpium against Glutamate-Induced HT22 Cell Cytotoxicity. (Pubmed Central) -  Dec 23, 2022   
    The administration of LY294002, a PI3K/Akt inhibitor, attenuated the neuroprotective effects of APE on oxidative stress-induced neuronal cell damage. This allowed us to infer that the protective effects of APE on oxidative damage to cells can be attributed to the PI3K/Akt-mediated Nrf-2/HO-1 signaling pathway.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Role of the CCL28-CCR10 pathway in monocyte migration in rheumatoid arthritis (Pubmed Central) -  Dec 20, 2022   
    CCL28 ligation to CCR10 promoted RA monocyte migration through activation of the ERK and PI3K/Akt signaling pathways. The CCL28-CCR10 pathway could participate in monocyte recruitment into RA joints, thereby contributing to synovial inflammation and bone destruction.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Role of the mTOR Signalling Pathway During Extracellular Acidosis in Tumour Cells. (Pubmed Central) -  Dec 18, 2022   
    The results of this study indicate that mTOR signalling is inhibited by extracellular acidosis which then lead to a reduced activity of the P70-S6 kinase (modulating gene expression) and increased autophagy possibly mediated by ULK1/2 activity. These finding may offer new perspectives for therapeutic interventions in acidic tumours.
  • ||||||||||  cisplatin / Generic mfg., dasatinib / Generic mfg.
    Journal:  Src inhibitor dasatinib sensitized gastric cancer cells to cisplatin. (Pubmed Central) -  Dec 17, 2022   
    Furthermore, transcriptome sequencing also confirmed that the PI3K/AKT pathway was involved in the anti-cancer effect of dasatinib or combined with cisplatin. Additionally, GC cells with higher Src activity (AGS) elicited more sensitive to dasatinib than lower cells (SGC7901 and MGC803), suggesting that the Src levels could be applied to pre-select patients who would benefit from dasatinib and/or combined with platinum compounds.
  • ||||||||||  MK-2206 / Merck (MSD), LY294002 / Eli Lilly
    Journal:  Lipid droplet accumulation and adipophilin expression in follicular thyroid carcinoma. (Pubmed Central) -  Dec 16, 2022   
    Immunohistochemical analysis of surgically resected human thyroid tissues revealed significantly increased expression of adipophilin in FTC compared with FTA and adjacent non-tumorous thyroid epithelia. Taken together, LDs and adipophilin were abundant in cultured FTC; the evaluation of adipophilin expression can help distinguish FTC from FTA in surgical specimens.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Sirt3 activates autophagy to prevent DOX-induced senescence by inactivating PI3K/AKT/mTOR pathway in A549 cells. (Pubmed Central) -  Dec 16, 2022   
    We here investigate how Sirt3 regulates doxorubicin (DOX)-induced senescence in lung cancer A549 cells...Importantly, the autophagy inhibitors 3-methyladenine (3-MA) and chloroquine (CQ) partially abolished the antioxidant stress and antiaging effects of Sirt3, while the autophagy activator rapamycin (Rap) potentiated these effects of Sirt3, demonstrating that autophagy mediates the anti-aging effects of Sirt3...The PI3K inhibitor LY294002 promoted the antioxidant stress and antiaging effects of Sirt3, while the AKT activator SC-79 reversed these effects of Sirt3. Taken together, Sirt3 counteracts DOX-induced senescence by improving autophagic flux.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Acteoside Derived from Cistanche Improves Glucocorticoid-Induced Osteoporosis by Activating PI3K/AKT/mTOR Pathway. (Pubmed Central) -  Dec 16, 2022   
    Additionally, ACT attenuated Dex-induced inhibition of p-AKT/AKT, p-mTOR/mTOR, and p-PI3K/PI3K protein levels by Dex (P < 0.05), while the PI3K/AKT/mTOR pathway inhibitor LY294002 diminished the potential effect of ACT (P < 0.05). ACT from Cistanche may exert osteoprotective effects by activating the PI3K/AKT/mTOR signaling pathway to alleviate Dex-induced osteoporosis.
  • ||||||||||  LY294002 / Eli Lilly
    Journal, IO biomarker:  Effects of matrine combined with LY294002 on proliferation, apoptosis and cell cycle of human myeloid leukemia K562 cells (Pubmed Central) -  Dec 13, 2022   
    ACT from Cistanche may exert osteoprotective effects by activating the PI3K/AKT/mTOR signaling pathway to alleviate Dex-induced osteoporosis. Matrine combined with LY294002 produces a synergistic inhibitory effect on K562 cells possibly by down-regulating the p-Akt expression in PI3K/Akt signaling pathway, reducing the expressions of p-mTOR, cyclinD1 and Bcl-2, and increasing the expression of caspase-9.
  • ||||||||||  LY294002 / Eli Lilly, selisistat (SEN-196) / AOP Orphan Pharma
    Journal:  Resveratrol Inhibits Insulin-Induced Vascular Smooth Muscle Cell Proliferation and Migration by Activating SIRT1. (Pubmed Central) -  Dec 9, 2022   
    A SIRT1 inhibitor, EX527, reversed the inhibitory effect of resveratrol on insulin-induced VSMC proliferation and migration and activation of PI3K and Akt phosphorylation levels. In conclusion, our study revealed that treatment with resveratrol inhibited insulin-mediated VSMC proliferation and migration, possibly by activating SIRT1 and downregulating the PI3K/AKT pathway.
  • ||||||||||  LY294002 / Eli Lilly, tilarginine (L-NMMA) / Arginox Pharma, Houston Methodist Research Institute
    Journal:  Effect of astragaloside Ⅳ on angiotensin Ⅱ-induced inflammatory response of vascular endothelial cells and mechanism (Pubmed Central) -  Dec 7, 2022   
    This study provides a direct link between AS-Ⅳ and Ca~(2+)/PI3K/Akt/eNOS/NO pathway in AS-Ⅳ-mediated anti-inflammatory actions in endothelial cells exposed to Ang Ⅱ. The results indicate that AS-Ⅳ attenuates endothelial cell-mediated inflammatory response induced by Ang Ⅱ via the activation of Ca~(2+)/PI3K/Akt/eNOS/NO signaling pathway.