LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  ADORA1 Promotes Hepatocellular Carcinoma Progression via PI3K/AKT Pathway. (Pubmed Central) -  Dec 10, 2020   
    Treatment with PI3K inhibitor LY294002 blocked the effects of ADORA1 on tumor growth in either ADORA1-overexpressing or -deficiency cells...Treatment of ADORA1 antagonist oppositely suppressed HCC xenograft tumor growth. ADORA1 serves as an important oncoprotein and a promoter of cell proliferation through PI3K/AKT signaling pathway in hepatocellular carcinoma.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Tuoyi (toripalimab) / Shanghai Junshi Biosci, rapamycin topical (PTX-022) / Palvella Therapeutics, Ligand
    Journal, PD(L)-1 Biomarker, IO Biomarker:  Apelin-13 inhibits apoptosis and excessive autophagy in cerebral ischemia/reperfusion injury. (Pubmed Central) -  Dec 5, 2020   
    Both LY294002 (20 μM) and rapamycin (500 nM), which are inhibitors of the PI3K/Akt/mTOR pathway, significantly attenuated the inhibition of autophagy and apoptosis caused by apelin-13...The study was approved by the Animal Ethical and Welfare Committee of Jining Medical University, China (approval No. 2018-JS-001) in February 2018.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Mozobil (plerixafor) / Sanofi, PD98059 / Wayne State University
    Journal:  Role of the stromal cell derived factor-1 in the biological functions of endothelial progenitor cells and its underlying mechanisms. (Pubmed Central) -  Dec 5, 2020   
    Moreover, SDF-1 significantly increased the protein expression levels of phosphorylated (p)-Akt and p-ERK; however, SDF-1-induced effects on protein expression were suppressed by AMD3100, LY294002 and PD98059. Thus, SDF-1-induced EPC proliferation was mediated by activation of the Akt and ERK signaling pathways, whereas SDF-1-mediated EPC migration and tube formation only involved activation of the Akt signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Klotho gene improves oxidative stress injury after myocardial infarction. (Pubmed Central) -  Dec 5, 2020   
    Further, the Klotho protein expression of the pDC316-Klotho group was significantly upregulated and the Nrf-2 and ARE proteins expressions of the LY294002 and pDC316-Klotho groups were significantly suppressed. Klotho overexpression improved findings of oxidative stress injury after myocardial infarction.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Cardioprotective effect exerted by Timosaponin BⅡ through the regulation of endoplasmic stress-induced apoptosis. (Pubmed Central) -  Dec 1, 2020   
    Taken together, these results demonstrated that curcumin protects SH‑SY5Y cells against OGD/R injury by inhibiting apoptosis and oxidative stress, and via enhancing the APE1 level and activity, promoting PI3K/AKT pathway activation. These results suggested that TBⅡ protects against myocardial injury in vitro and enhances cellular defense capacity by inhibiting ER stress-mediated apoptosis pathways in vivo by activating the PI3K/Akt pathways.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Proliferation and invasion of ovarian cancer SK-OV-3 cells inhibited by Tectoridin (Pubmed Central) -  Dec 1, 2020   
    Compared with the control group, the difference in the LY294002 group was statistically significant (P<0.05). Tectoridin may inhibit proliferation, migration and invasion of SK-OV-3 cells by regulating PI3K/AKT signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Neural maturation enhanced by exercise-induced extracellular derivatives. (Pubmed Central) -  Nov 26, 2020   
    Finally, the administration of exercise-induced EDs for 3 days increased the Histone 3 phosphorylation and β-III tubulin expression in Ink/Arf null neural stem cells and progenitors (NSPCs) under each proliferation and differentiation condition. These results suggest that exercise-induced circulating EDs may mediate neuronal maturation during exercise.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Biomarker, Preclinical, Journal:  Berberine ameliorates renal impairment and inhibits podocyte dysfunction by targeting the PI3K/Akt pathway in diabetic rat. (Pubmed Central) -  Nov 25, 2020   
    These results suggest that exercise-induced circulating EDs may mediate neuronal maturation during exercise. Berberine could be a promising antidiabetic nephropathy drug through ameliorating renal impairment and inhibiting podocyte dysfunction in diabetic rats, and the underlying molecular mechanisms might be involved in the regulation of the PI3K-Akt signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Endothelial Nitric Oxide Mediates the Anti-Atherosclerotic Action of Torenia concolor Lindley var. Formosama Yamazaki. (Pubmed Central) -  Nov 25, 2020   
    Moreover, TCEE-induced NO production, and EC proliferation, migration, and tube formation were diminished by pretreatment with LY294002 (an Akt inhibitor), KN62 (a CaMKII inhibitor), and compound C (an AMPK inhibitor)...Moreover, chronic treatment with TCEE attenuated hyperlipidemia, systemic and aortic inflammatory response, and the atherosclerotic lesions in apolipoprotein E-deficient mice. Collectively, our findings suggest that TCEE may confer protection from atherosclerosis by preventing endothelial dysfunction.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  CCN5 inhibits proliferation and promotes apoptosis of oral squamous cell carcinoma cells. (Pubmed Central) -  Nov 21, 2020   
    Further, LY294002, a PI3K/AKT antagonist, was employed to explore the mechanism underlying the effects of CCN5 in the regulation of OSCC...Finally, xenograft analysis showed that CCN5 represses tumorigenesis of OSCC cells. These findings together suggest that CCN5 functions as a tumor suppressor for OSCC cell development through inactivation of PI3K/AKT signaling pathway, providing a potential candidate for OSCC therapy.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Role of Lysophosphatidic Acid in Vascular Smooth Muscle Cell Proliferation. (Pubmed Central) -  Nov 19, 2020   
    Furthermore, gene expressions for PLC β1 isoform, PKC δ and ε isoforms, casein kinase II β isoform and endothelin-1A receptors were elevated by LPA. These results suggest that the LPA-induced proliferation of VSM cells is mediated through the activation of GPCR and multiple protein kinases as well as gene expressions of their some specific isoforms.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  Nano-silicon Dioxide Affects Apoptosis of Alveolar Macrophages via PI3K/AKt Signaling Pathway (Pubmed Central) -  Nov 18, 2020   
    With LY294002 pretreatment, the mitochondrial transmembrane potential level and the expressions of p-PI3K, p-AKt and Bcl-2 were decreased, the expression of Bax and the apoptosis rate were increased. Our data suggested that the activation of PI3K/AKt signaling pathway played an important role in NS-induced apoptosis in alveolar macrophages.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega, SP600125 / BMS
    Journal, PARP Biomarker, IO Biomarker:  Morusin induces apoptosis and autophagy via JNK, ERK and PI3K/Akt signaling in human lung carcinoma cells. (Pubmed Central) -  Nov 12, 2020   
    A PI3K/Akt inhibitor (LY294002), a JNK inhibitor (SP60015) and a MEK/ERK inhibitor (U0126) contributed to the determination that these pathways were involved in both apoptosis and autophagy induced by morusin. Moreover, morusin treatment strikingly enhanced intracellular ROS level, an ROS scavenger NAC blocked cell death and changes of Akt, JNK and ERK induced by morusin.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, PARP Biomarker:  Capillarisin protects SH-SY5Y cells against bupivacaine-induced apoptosis via ROS-mediated PI3K/PKB pathway. (Pubmed Central) -  Nov 6, 2020   
    Together, our results provide foundation for further development of safer and more effective glucocorticoid-based combination therapy of hematological malignancies using PI3K/Akt/mTOR inhibitors. Capillarisin protected SH-SY5Y cells against bupivacaine-induced apoptosis by inhibiting oxidative stress, mitochondrial injury, and endoplasmic reticulum stress via ROS-mediated of PI3K/PKB pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Transcriptomics predicts compound synergy in drug and natural product treated glioblastoma cells. (Pubmed Central) -  Nov 6, 2020   
    Furthermore, in combination, fucoxanthin synergizes with LY-294002 in inhibiting the growth of U87MG cells, suggesting complementarity in their molecular modes of action and pointing to further treatment combinations. The synergy we observe between the dietary nutraceutical fucoxanthin and the synthetic chemical LY-294002 in producing growth arrest in glioblastoma, illustrates the potential of nutri-pharmaceutical combinations in targeting this challenging disease.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    [VIRTUAL] Thrombopoietin Protects Neural Cells and Endothelial Cells from Apoptosis Via PI3K/AKT Pathway (Poster Hall (Virtual Meeting)) -  Nov 5, 2020 - Abstract #ASH2020ASH_3456;    
    LY-294002 pretreatment suppressed the TPO-induced AKT activation and abolished the prosurvival effect of TPO... TPO has a protective effect against apoptosis of neural cells and endothelial cells through activating the PI3K/AKT pathway, thus decreasing the expression of apoptosis protease Caspase-3 and inhibiting the reduction of MMP.
  • ||||||||||  Ibrance (palbociclib) / Pfizer, quercetin (LY294002) / Eli Lilly, Verzenio (abemaciclib) / Eli Lilly
    [VIRTUAL] Autophagy Inhibition Enhances CDK4/6 Inhibitor-Induced Apoptosis in t(8;21) Acute Myeloid Leukemia Cells (Poster Hall (Virtual Meeting)) -  Nov 5, 2020 - Abstract #ASH2020ASH_807;    
    Because CCND2 is not a druggable target, we examined the effect of CDK4/6 inhibitors (palbociclib and abemaciclib) on t(8;21) AML cells...Treatment of t(8;21) AML cells with the autophagy inhibitors chloroquine (CQ) or LY294002 in combination with abemaciclib significantly increased the frequency of apoptotic (Annexin V positive) cells compared with that in untreated cells, whereas CQ or LY294002 single treatment had no significant effect on apoptosis...These results suggest that autophagy inhibition enhances CDK4/6 inhibitor-induced apoptosis in t(8;21) AML cells. In conclusion, the present results indicate that inhibition of CDK4/6 and autophagy may be a novel and promising biomarker-driven therapeutic strategy for the treatment of t(8;21) AML.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega
    [VIRTUAL] RASA3 Regulates Stage-Specific AKT Signaling and Cell Cycle Progression in Mammalian Erythropoiesis (Channel 5 (Virtual Meeting)) -  Nov 5, 2020 - Abstract #ASH2020ASH_755;    
    This suggests a dynamic relationship between RASA3, Ras signaling, and cell cycle progression throughout early and late erythroid differentiation. Together, these findings support the role of RASA3 as a regulator of the signaling networks governing erythropoiesis and reveal a new targetable axis in a model of inherited bone marrow failure.
  • ||||||||||  pegylated recombinant human arginase (BCT-100) / BCT international, quercetin (LY294002) / Eli Lilly
    Journal:  Contactin 1 modulates pegylated arginase resistance in small cell lung cancer through induction of epithelial-mesenchymal transition. (Pubmed Central) -  Nov 4, 2020   
    Silencing CNTN-1 rather than CDH17 or IGF2BP1 in H446-BR and H526-BR cells re-sensitized resistant cells to BCT-100 treatment and attenuated the epithelial-mesenchymal transition (EMT) phenotype. The AKT signaling pathway was activated in H446-BR and H526-BR cells accompanied by EMT progression, and AKT inhibitor LY294002 reversed the EMT progression in resistant cells.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  Chrysin enhances anticancer drug-induced toxicity mediated by the reduction of claudin-1 and 11 expression in a spheroid culture model of lung squamous cell carcinoma cells. (Pubmed Central) -  Nov 2, 2020   
    LY-294002, an inhibitor of phosphatidylinositol 3-kinase, inhibited the phosphorylation of Akt and decreased the expression levels of CLDN1 and CLDN11...The knockdown of CLDN1 and CLDN11 using small interfering RNAs increased the transepithelial flux of doxorubicin (DXR), an anthracycline anticancer drug...Taken together, chrysin may bind to Akt and inhibit its phosphorylation, resulting in the elevation of anticancer drug-induced toxicity mediated by reductions in CLDN1 and CLDN11 expression in RERF-LC-AI cells. We suggest that chrysin may be useful as an adjuvant chemotherapy in lung SCC.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Mitochondrial dysfunction increases pro-inflammatory cytokine production and impairs repair and corticosteroid responsiveness in lung epithelium. (Pubmed Central) -  Nov 2, 2020   
    The reduced corticosteroid responsiveness may be mediated by glycolytic reprogramming, specifically glycolysis-associated PI3K signaling, as PI3K inhibitor LY294002 restored the sensitivity of CXCL8 secretion to corticosteroids in A549 Rho-0 cells. In conclusion, mitochondrial defects may lead to increased lung epithelial pro-inflammatory responses, reduced epithelial repair and reduced corticosteroid responsiveness in lung epithelium, thus potentially contributing to the pathogenesis of COPD.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega
    Journal:  The Neurotrophic Function of Glucagon-Like Peptide-1 Promotes Human Neuroblastoma Differentiation via the PI3K-AKT Axis. (Pubmed Central) -  Oct 30, 2020   
    PI3K inhibitor (LY294002) and MEK inhibitor (U0126) were used to determine the signaling pathway in regulation of neuronal differentiation. The sequential treatment of retinoic acid and GLP-1 within a serum-free medium is able to trigger the differentiation of SH-SY5Y cells into morphologically and physiologically mature glutamatergic and dopaminergic neurons.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Mechanical stress promotes biological functions of C2C12 myoblasts by activating PI3K/AKT/mTOR signaling pathway. (Pubmed Central) -  Oct 28, 2020   
    The PI3K specific inhibitor LY294002 significantly decreased 4EBP1 expression and reduced p‑AKT and p‑mTOR expression compared with the mechanical stress group...In conclusion, mechanical stress promoted biological functions of C2C12 cells by activating the PI3K/AKT signaling pathway. These results may contribute to a better understanding of the effects of mechanical stress on cells.