LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  CPA4 Promotes EMT in Pancreatic Cancer via Stimulating PI3K-AKT-mTOR Signaling. (Pubmed Central) -  Sep 16, 2020   
    However, LY294002 reversed CPA4 overexpression-stimulated cell proliferation and drug resistance in vitro in Bcl2/Bax and caspase3-dependent apoptosis. CPA4 overexpression contributes to aggressive clinical stage of PC patients and promotes EMT in vitro via activation of PI3K-AKT-mTOR signaling.
  • ||||||||||  dipyridamole / Generic mfg., quercetin (LY294002) / Eli Lilly, U0126 / Promega
    Journal:  Anti‑platelet activity of mineral‑balanced deep sea water is mediated via the regulation of Akt and ERK pathway crosstalk. (Pubmed Central) -  Sep 13, 2020   
    Taken together, the results of the present investigation suggest that the inhibitory effects of MBDSW on platelet aggregation may be associated with the cross‑inhibition of Akt and ERK phosphorylation. These results strongly indicate that MBDSW may have preventive or therapeutic potential for platelet aggregation‑mediated diseases, such as thrombosis, atherosclerosis and myocardial infarction.
  • ||||||||||  MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly
    Journal:  PI3K/Akt/FoxO pathway mediates glycolytic metabolism in HepG2 cells exposed to triclosan (TCS). (Pubmed Central) -  Sep 13, 2020   
    The PI3K/Akt/FoxO pathway was identified to play a pivot role in TCS-induced glycolysis, which was further confirmed by inhibitor tests using specific inhibitors LY294002 and MK2206. In general, TCS can induce oxidative stress, cause oxidative damages and promote glycolysis in HepG2 cells, which was mediated by the PI3K/Akt/FoxO pathway.
  • ||||||||||  dexamethasone / Generic mfg., quercetin (LY294002) / Eli Lilly
    Journal:  Involvement of claudin-5 in HS-induced acute lung injury. (Pubmed Central) -  Sep 13, 2020   
    Moreover, as a consequence of the altered phosphorylation of AKT and FoxO1, a change in claudin-5 with the same trend was observed. Therefore, the tight junction protein claudin-5 might be considered a therapeutic target for the treatment of ALI induced by HS and other hazardous gases.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Artesunate Ameliorates Sepsis-Induced Acute Lung Injury by Activating the mTOR/AKT/PI3K Axis. (Pubmed Central) -  Sep 10, 2020   
    The rats were randomly assigned into 4 groups: Sham, LPS, LPS + AS, and LPS + AS + LY294002...AS could partially protect against LPS-induced ALI by inhibiting apoptosis and inflammatory mediator production, and this function is perhaps associated with the regulation of the mTOR/AKT/PI3K axis. These findings suggest that AS may possess certain beneficial characteristics in protecting the lungs from sepsis.
  • ||||||||||  MK-2206 / Merck (MSD), bleomycin / Generic mfg., BMS, quercetin (LY294002) / Eli Lilly
    Journal:  PTEN loss regulates alveolar epithelial cell senescence in pulmonary fibrosis depending on Akt activation. (Pubmed Central) -  Sep 9, 2020   
    These indicated that senescent AECs modulated by the PTEN/Akt pathway promote lung fibrosis. In conclusion, our study demonstrated that as a trigger indicator in IPF, the senescence process in AECs should be a potential therapeutic target and that the PTEN/Akt pathway may be a promising candidate for intervention.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Icariin Protects Mouse Insulinoma Min6 Cell Function by Activating the PI3K/AKT Pathway. (Pubmed Central) -  Sep 5, 2020   
    The effects of ICA and UA on the PI3K/Akt pathway were also analyzed by western blotting, as were the effects of the specific PI3K/Akt inhibitor LY294002...CONCLUSIONS ICA protected Min6 cell function, an effect likely mediated by the PI3K pathway. ICA may inhibit the progression of diabetes.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Involvement of CaMKII in regulating the release of diplotene-arrested mouse oocytes by pAkt1 (Ser473). (Pubmed Central) -  Sep 4, 2020   
    On the contrary, down-regulation of PIP3 by LY294002 decreased GVBD rates and the levels of pCaMKII (Thr286) and pAkt1 (Ser473), respectively. Our results showed that Akt1 and CaMKII regulated each other, and PIP3 may be involved in these regulations during the release of mouse oocytes from diplotene arrest.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  Cryptotanshinone inhibits hypoxia/reoxygenation-induced oxidative stress and apoptosis in renal tubular epithelial cells. (Pubmed Central) -  Sep 2, 2020   
    Furthermore, CTS activated the levels of p-PI3K and p-Akt in H/R-injured HK-2 cells; meanwhile, the renal protective activity of CTS was inhibited by the inhibitor of the (phosphatidylinositol 3 kinase/protein kinase B) PI3K/Akt pathway (LY294002). These findings indicate that CTS can ameliorate renal I/R injury in vitro partly through regulating the PI3K/Akt pathway.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Acteoside inhibits autophagic apoptosis of retinal ganglion cells to rescue glaucoma-induced optic atrophy. (Pubmed Central) -  Sep 2, 2020   
    These findings indicate that CTS can ameliorate renal I/R injury in vitro partly through regulating the PI3K/Akt pathway. In summary, we conclude that Acteoside inhibits autophagy-induced apoptosis in RGCs through the OPTN and PI3K/AKT/mTOR pathway, and glaucoma patients may benefit from Acteoside treatment alone or in combination with other autophagy inhibitors.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University, SP600125 / BMS
    Biomarker, Preclinical, Journal:  Hepatoma-derived growth factor enhances osteoblastic transformation of rat aortic vascular smooth muscle cells in vitro. (Pubmed Central) -  Sep 1, 2020   
    In summary, we conclude that Acteoside inhibits autophagy-induced apoptosis in RGCs through the OPTN and PI3K/AKT/mTOR pathway, and glaucoma patients may benefit from Acteoside treatment alone or in combination with other autophagy inhibitors. In conclusion, in synergism with other osteogenic factor, HDGF may promote the progression of osteobastic transformation of VSMCs via Akt and p38 signaling pathways and contribute to vascular calcification in arteriosclerosis.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Protective effect of insulin on burn serum-challenged cardiomyocytes in vitro (Pubmed Central) -  Sep 1, 2020   
    In conclusion, in synergism with other osteogenic factor, HDGF may promote the progression of osteobastic transformation of VSMCs via Akt and p38 signaling pathways and contribute to vascular calcification in arteriosclerosis. For cardiomyocytes challenged by burn serum, insulin may decrease inflammation, apoptosis and then protect the cardiomyocytes.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Leptin receptor mediates the proliferation and glucose metabolism of pancreatic cancer cells via AKT pathway activation. (Pubmed Central) -  Aug 29, 2020   
    In addition, the effects of leptin stimulation were significantly counteracted by the AKT inhibitor LY294002, whereas the effects of leptin silencing were counteracted by AKT activator insulin‑like growth factor 1. The results of the present study suggested that leptin may contribute to cell proliferation and glucose metabolism of human PC cells, which may be through activation of the AKT pathway.
  • ||||||||||  metformin / Generic mfg.
    Journal:  AICAR Stimulates the Pluripotency Transcriptional Complex in Embryonic Stem Cells Mediated by PI3K, GSK3β, and β-Catenin. (Pubmed Central) -  Aug 26, 2020   
    According to our findings, we provide a mechanism by which AICAR increases and maintains a pluripotency state through enhanced Nanog expression, involving AMPK/PI3K and p-GSK3β Ser21/9 pathways backing up the AICAR function as a potential target for this drug controlling pluripotency. The highlights of this study are that AICAR (5-aminoimidazole-4-carboxamied-1-b-riboside), an AMP protein kinase (AMPK) activator, blocks the ESC differentiation and AMPK is a key enzyme for pluripotency and shows valuable data to clarify the molecular pluripotency mechanism.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  The PI3K/Akt pathway is not a main driver in HDL-mediated cell protection. (Pubmed Central) -  Aug 23, 2020   
    In the three cellular models, LY294002, a PI3K inhibitor, only slightly blunted HDLs protection, indicating that HDLs induce PI3K-independent cell protection...This study demonstrates that the PI3K-Akt signaling pathway is not the main mediator of the cell protective functions of HDLs. Further investigation is therefore needed to identify the intrinsic mechanism of HDL-mediated cell protection.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Belsomra (suvorexant) / Merck (MSD)
    Journal, IO Biomarker:  Orexin-A protects against oxygen-glucose deprivation/reoxygenation-induced cell damage by inhibiting endoplasmic reticulum stress-mediated apoptosis via the Gi and PI3K signaling pathways. (Pubmed Central) -  Aug 23, 2020   
    In addition, in order to prove the specificity of these characteristics, the OXA antagonist Suvorexant (DORA; Ki of 0.55 nM and 0.35 nM for OX1R and OX2R) was used for intervention...Collectively, our results indicate that OXA has a neuroprotective effect on OGD/R-induced cell damage by inhibiting ERS-induced apoptosis through the combined action of Gi and PI3K signaling pathways. These findings help to clarify the mechanism underlying the neuroprotective action of OXA, which should aid the development of further candidate drugs, and provide a new therapeutic direction for the treatment of ischemic stroke.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  Qishen Yiqi Drop Pill, a novel compound Chinese traditional medicine protects against high glucose-induced injury in cardiomyocytes. (Pubmed Central) -  Aug 23, 2020   
    These findings help to clarify the mechanism underlying the neuroprotective action of OXA, which should aid the development of further candidate drugs, and provide a new therapeutic direction for the treatment of ischemic stroke. In summary, these findings demonstrated that QSYQ effectively protected H9c2 cells against the series injuries due to high glucose at least partially by activating the PI3K/Akt signalling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, GLG-302 / GLG Pharma
    Preclinical, Journal:  Targeting the PI3K/STAT3 axis modulates age-related differences in macrophage phenotype in rats with myocardial infarction. (Pubmed Central) -  Aug 23, 2020   
    Furthermore, LY294002 abolished the STAT3 phosphorylation, whereas PI3K activity was not affected following the inhibition of STAT3. In conclusions, the host environment is responsible for ageing-related myofibroblast dysregulation in response to MI which can be improved by administering n-butylidenephthalide via macrophage differentiation towards M2 phenotype by targeting the PI3K/STAT3 axis.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Sesamin suppresses NSCLC cell proliferation and induces apoptosis via Akt/p53 pathway. (Pubmed Central) -  Aug 23, 2020   
    When Akt and p53 were suppressed by LY294002 and PFTα, respectively, sesamin exerted no additional effects...Taken together, this study demonstrates that sesamin suppresses NSCLC cell proliferation by induction of G1 phase cell cycle arrest and apoptosis via Akt/p53 pathway. Therefore, sesamin may be a promising adjuvant treatment for NSCLC therapy.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  CCL18 promotes the invasion and metastasis of breast cancer through Annexin A2. (Pubmed Central) -  Aug 23, 2020   
    In brief, AnxA2, as a downstream molecule of Nir 1 binding to CCL18, promotes invasion and metastasis by EMT through the PI3K/Akt/GSK3β/Snail signaling pathway in breast cancer. This study suggests that AnxA2 is a potential anti‑invasion/metastasis target for therapeutic intervention in breast cancer.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, gefitinib / Generic mfg., SCH772984 / Otsuka
    Journal, IO Biomarker:  JuBei Oral Liquid Induces Mitochondria-Mediated Apoptosis in NSCLC Cells. (Pubmed Central) -  Aug 22, 2020   
    Moreover, JB could synergize with gefitinib to induce apoptosis in PC-9, PC-9/GR and H1975 cells. These data indicated that JB could be a potential therapeutic agent for NSCLC patients harboring EGFR mutations as well as those under gefitinib resistance.
  • ||||||||||  tacrolimus / Generic mfg.
    Journal:  Ginseng increases Klotho expression by FoxO3-mediated manganese superoxide dismutase in a mouse model of tacrolimus-induced renal injury. (Pubmed Central) -  Aug 20, 2020   
    In the mitochondria, ginseng reduced mitochondrial reactive oxygen species production, mitochondrial membrane potential, and oxygen consumption rate, whereas blocking phosphatidylinositol 3-kinase activity with LY294002 enhanced them. These findings together suggested that ginseng attenuated tacrolimus-induced oxidative stress via signaling between Klotho and the phosphatidylinositol 3-kinase/serine-threonine kinase Akt/forkhead box protein O3a-related antioxidant pathway.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  Effect of Bmi-1 on Multidrug Resistance in K562/ADR Cells and Its Mechanisms (Pubmed Central) -  Aug 19, 2020   
    These findings together suggested that ginseng attenuated tacrolimus-induced oxidative stress via signaling between Klotho and the phosphatidylinositol 3-kinase/serine-threonine kinase Akt/forkhead box protein O3a-related antioxidant pathway. Bmi-1 plays a key role in MDR-mediated multidrug resistance in K562/ADR cells, which may be mediated by activating PTEN/AKT pathway to regulate NF-κB.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, docetaxel / Generic mfg.
    Journal:  PLGA nanoparticle-based docetaxel/LY294002 drug delivery system enhances antitumor activities against gastric cancer. (Pubmed Central) -  Aug 14, 2020   
    Histological analysis indicated that PLGA(TXT+LY294002) was biocompatible and had no toxicity to major organs. Characterized by the combined slow release of TXT and LY294002, this novel PLGA-based TXT/LY294002 drug delivery system provides controlled release and tumor targeting and is safe, shedding light on the future of targeted therapy against GC.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal, IO Biomarker:  Administration of rCTRP9 Attenuates Neuronal Apoptosis Through AdipoR1/PI3K/Akt Signaling Pathway after ICH in Mice. (Pubmed Central) -  Aug 11, 2020   
    To elucidate the underlying mechanisms, adiponectin receptor1 small interfering ribonucleic acid (AdipoR1 siRNA) and selective PI3 K inhibitor LY294002 were administered prior to rCTRP9 treatment...Administration of rCTRP9 significantly improved both short- and long-term neurofunctional behavior after ICH. RCTRP9 treatment significantly increased the expression of AdipoR1, PI3 K, p-Akt, and Bcl-2, while at the same time was found to decrease the expression of Bax in the brain, which was reversed by inhibition of AdipoR1 and PI3 K. The neuroprotective effect of rCTRP9 after ICH was mediated by attenuation of neuronal apoptosis via the AdipoR1/PI3K/Akt signaling pathway; therefore, rCTRP9 should be further evaluated as a potential therapeutic agent for ICH patients.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, BRCA Biomarker:  The Interaction of PI3K Inhibition with Homologous Recombination Repair in Triple Negative Breast Cancer Cells. (Pubmed Central) -  Aug 11, 2020   
    RCTRP9 treatment significantly increased the expression of AdipoR1, PI3 K, p-Akt, and Bcl-2, while at the same time was found to decrease the expression of Bax in the brain, which was reversed by inhibition of AdipoR1 and PI3 K. The neuroprotective effect of rCTRP9 after ICH was mediated by attenuation of neuronal apoptosis via the AdipoR1/PI3K/Akt signaling pathway; therefore, rCTRP9 should be further evaluated as a potential therapeutic agent for ICH patients. Consequently, targeted therapies based on the interaction of PI3K inhibition with BRCA1 mutations or HR deficiency in TNBC may be a promising strategy for the treatment of patients with TNBC.