LY294002 / Eli Lilly 
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  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Alpinae Oxyphyllae Fructus alleviated LPS-induced cognitive impairments via PI3K/AKT/NF-κB signaling pathway. (Pubmed Central) -  Feb 3, 2022   
    Additionally, we discovered that AOF could significantly decrease the high expression of cytokines as well as the expression and translocation of NF-κB induced by LPS in PC12 cells. These results demonstrate the anti-neuroinflammatory effect of AOF in both cell and animal models of AD, thereby slowing down the process and development of the disease.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  CWHM-1008 Induces Apoptosis and Protective Autophagy through the Akt/mTOR Axis in LUAD Cells. (Pubmed Central) -  Feb 1, 2022   
    Potential effects of an autophagy inhibitor (LY294002) and constitutively active Akt plasmid (CA-Akt) on CWHM-1008-induced apoptosis were also examined...Moreover, CWHM-1008 significantly inhibited the growth and induced apoptosis of A549 cell in nude mice in vivo. The present findings provide new insights into anticancer properties of CWHM-1008, suggesting that it may be an adjuvant treatment for LUAD treatment, warranting further study.
  • ||||||||||  LY294002 / Eli Lilly, dorsomorphin (Compound C) / EMD Serono
    Journal, PARP Biomarker:  Arsenic induces autophagy-dependent apoptosis via Akt inactivation and AMPK activation signaling pathways leading to neuronal cell death. (Pubmed Central) -  Jan 29, 2022   
    Expectedly, inhibition of Akt signaling with LY294002 obviously enhanced As-triggered autophagy and apoptosis...Taken together, these results indicated that As exerted its cytotoxicity in neuronal cells via the Akt inactivation/AMPK activation downstream-regulated autophagy-dependent apoptosis pathways, which ultimately lead to cell death. Our findings suggest that the regulation of Akt/AMPK signals may be a promising intervention to against As-induced neurotoxicity and NDs.
  • ||||||||||  LY294002 / Eli Lilly
    Preclinical, Journal:  PI3K/AKT pathway mediates the antidepressant- and anxiolytic-like roles of hydrogen sulfide in streptozotocin-induced diabetic rats via promoting hippocampal neurogenesis. (Pubmed Central) -  Jan 29, 2022   
    Furthermore, inhibited PI3K/AKT pathway by LY294002 significantly abolished HS-exerted the improvement of hippocampal neurogenesis and the antidepressant- and anxiolytic-like effects in the STZ-induced diabetic rats. Taken together, these results uncover that the activation of hippocampal PI3K/AKT pathway plays an important role to restore hippocampal neurogenesis and subsequently to mediate the antidepressant- and anxiolytic-like roles of HS in STZ-induced diabetic rats and enhance our understanding of the robustness of HS as a therapeutic strategy for treatment of depression in diabetes mellitus.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Hemocyte extracellular traps of Manila clam Ruditapes philippinarum: Production characteristics and antibacterial effects. (Pubmed Central) -  Jan 27, 2022   
    Furthermore, ET production could be inhibited by phosphotidylinsitol-3-kinase (PI3K) inhibitor (LY294002) and extracellular regulated protein kinase (ERK) inhibitor (U0126), suggesting the idea that both the PI3K and ERK pathways were suggested to function during ETosis...Furthermore, our scanning electron microscopy (SEM) observation and antibacterial activities test successfully showed the patterns how clam ETs entrapped and killed the invading V. anguillarum. Taken together, our results revealed that ETosis with bactericidal effect increased ROS, MPO and glycolysis level and carried out in a ROS-, MPO-, PI3K-ERK-dependent manner.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Methyl eugenol attenuates liver ischemia reperfusion injury via activating PI3K/Akt signaling. (Pubmed Central) -  Jan 27, 2022   
    Our findings support the hypothesis that inhibitors of mTOR and PI3K might be an attractive tool to delay primordial follicle activation induced by cryopreservation and culture, thus preserving the ovarian reserve while retaining follicles in a functionally integrated state. The use of ME is a potential therapeutic approach for regulating LIRI by activating PI3K/Akt signaling.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Salvianolic acid B attenuates oxidative stress-induced injuries in enterocytes by activating Akt/GSK3β signaling and preserving mitochondrial function. (Pubmed Central) -  Jan 27, 2022   
    Mechanistically, Sal B treatment up-regulated the phosphorylated level of Akt and GSK3β in enterocytes in vitro and in vivo, and PI3K inhibitor LY294002 treatment abrogated the protective effects of Sal B. Meanwhile, the inactivation of GSK3β reversed the oxidative stress-induced apoptosis and mitochondrial dysfunction in IEC-6 cells. Together, our results demonstrated that the damage of intestinal epithelial cells in in vitro and in vivo models were both attenuated by Sal B treatment, and such antioxidant activity might very possibly be attributed to the activation of Akt/GSK3β signaling.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Protective effect of sargahydroquinoic acid against Aβ-evoked damage via PI3K/Akt mediated Nrf2 antioxidant defense system. (Pubmed Central) -  Jan 27, 2022   
    Co-treatment with SHQA and LY294002, a specific PI3K inhibitor, inhibited nuclear Nrf2 expression and Akt phosphorylation, demonstrating that SHQA-mediated Nrf2 activation was directly associated with the PI3K/Akt signaling pathway...In silico docking simulation revealed that SHQA established specific interactions with the key amino acid residues of PI3K, Akt, and Nrf2-Keap1 via hydrogen bonding and van der Waals interactions, which may affect the biological capacities of target markers. Overall, this is the first report of this novel mechanism of SHQA as a Nrf2 activator against Aβ-mediated oxidative damage, suggesting that the compound might be a potential agent for the prevention of AD.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Rapamycin attenuates PLA2R activation-mediated podocyte apoptosis via the PI3K/AKT/mTOR pathway. (Pubmed Central) -  Jan 27, 2022   
    We demonstrated that podocyte apoptosis was induced by Group IB secretory phospholipase A2 (sPLA2IB) in a concentration- and time-dependent manner via upregulation of phosphoinositide 3-kinase (PI3K), protein kinase B (AKT), and mTOR, and inhibited by rapamycin or LY294002...The therapeutic implications of our findings are that strategies to reduce PLA2R activation and PI3K/AKT/mTOR pathway inhibition in PLA2R-activated podocytes help protect podocytes from apoptosis. The therapeutic potential of rapamycin shown in this study provides cellular evidence supporting the repurposing of rapamycin for MN treatment.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Endogenous regulation of the Akt pathway by the aryl hydrocarbon receptor (AhR) in lung fibroblasts. (Pubmed Central) -  Jan 27, 2022   
    There was no significant decrease in cell viability in Ahr MLFs treated with LY294002-a PI3K inhibitor-although LY294002 did attenuate MTT reduction, indicating an affect on mitochondrial function...In conclusion, Ahr ablation increased basal Akt phosphorylation in MLFs. Our results indicate that AhR may modulate the phosphorylation of a variety of novel proteins not previously identified as AhR targets, findings that help advance our understanding of the endogenous functions of AhR.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  Notoginsenoside R2 induces colonic microvascular injuries via regulating the Rap1GAP/PI3K/Akt signaling pathway. (Pubmed Central) -  Jan 26, 2022   
    The mechanism of NGR2 in angiogenesis was assessed by VEGFA165, LY294002, silencing, and overexpression plasmids of Rap1GAP in vitro...Furthermore, the cell viability, proliferation, and tube formation of pHUVECs were inhibited by NGR2 via blocking the Rap1GAP/PI3K/Akt signaling pathway. NGR2 could induce colonic mucosal microvascular injuries and promoted the intracellular glycolysis of pHUVECs via blocking the Rap1GAP/PI3K/Akt signaling pathway.
  • ||||||||||  LY294002 / Eli Lilly, PD98059 / Wayne State University
    Journal, PARP Biomarker, IO biomarker:  Harmine Hydrochloride Triggers G2/M Cell Cycle Arrest and Apoptosis in HCT116 Cells through ERK and PI3K/AKT/mTOR Signaling Pathways. (Pubmed Central) -  Jan 21, 2022   
    Furthermore, HMH reduced the levels of p-ERK, p-PI3K, p-AKT, and p-mTOR in HCT116 cells, and significantly inhibited p-ERK and p-AKT expression in cells treated with of HMH and PD98059, an ERK inhibitor, or LY294002, an AKT inhibitor (P<0.05 and P<0.01). These results demonstrate the inhibi-tory effect of HMH on cell proliferation and migration through inducing apoptosis by inhibiting ERK and PI3K/AKT/mTOR signaling pathways, indicating its potential therapeutic applications in CRC.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  PIM1 Inhibition Affects Glioblastoma Stem Cell Behavior and Kills Glioblastoma Stem-like Cells. (Pubmed Central) -  Jan 20, 2022   
    Treatment of neurospheres with PIM1 inhibitors (TCS PIM1-1, Quercetagetin, and LY294002) diminished the cell viability associated with reduced DNA synthesis rate, increased caspase 3 activity, decreased PCNA protein expression, and reduced neurosphere formation. Our results indicate that PIM1 affects the glioblastoma stem cell behavior, and its inhibition kills glioblastoma stem-like cells, pointing to PIM1 targeting as a potential anti-glioblastoma therapy.
  • ||||||||||  Focus V (anlotinib) / Advenchen, Sino Biopharm
    Journal, IO biomarker:  Anlotinib Overcomes Multiple Drug Resistant Colorectal Cancer Cells via Inactivating PI3K/AKT Pathway. (Pubmed Central) -  Jan 18, 2022   
    Taken together, our findings suggest that SOX2-OT regulates PAI-1-induced TNBC cell metastasis through miR-942-5p/PIK3CA signaling and illustrate the great potential of developing new SOX2-OT-targeting therapy for TNBC patients. Anlotinib inhibited the proliferation, migration, invasion and induced apoptosis of HCT-8/5-FU cells, and the mechanisms may be that anlotinib conquered multidrug resistance of colorectal cancer cells via inactivating of PI3K/AKT pathway.
  • ||||||||||  LY294002 / Eli Lilly
    Journal, IO biomarker:  Potentilla anserine L. polysaccharide inhibits cadmium-induced neurotoxicity by attenuating autophagy. (Pubmed Central) -  Jan 18, 2022   
    Furthermore, the PI3K inhibitor (LY294002 or 3-MA) and/or PAP reversed the Cd-induced upregulated expression of LC3 II, Beclin-1, and PI3K class III, with a synergy between PI3K inhibitor and PAP against Cd-induced autophagy. The findings suggested that PAP partially prevented Cd-induced autophagic cell death in neurons by inhibiting the PI3K class III/Beclin-1 signaling pathway in vitro and in vivo.
  • ||||||||||  perifosine (D21266) / AEterna Zentaris, LY294002 / Eli Lilly
    Journal:  Properties and regulation of Gly-Sar uptake and transport in bovine intestinal epithelial cells. (Pubmed Central) -  Jan 14, 2022   
    PI3K and AKT inhibitors were found to significantly suppress the expression of PepT1, thus impairing uptake and transport of Gly-Sar-FITC. Findings of this study thus suggest that the uptake and transport of Gly-Sar-FITC in BIECs are mediated by PepT1, and the PI3K/AKT signalling pathway regulates the absorption of small peptides.