LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Trp53 regulates platelets in bone marrow via the PI3K pathway. (Pubmed Central) -  Aug 9, 2020   
    In summary, PLTs were altered in p53 mice, and the PI3K signaling pathway was involved in that process, suggesting that the p53-dependent PI3K signaling pathway is involved in thrombocytopenia or PLT diseases. PLT number is reduced in p53 deficiency; however, this reduction could be reverted by inhibiting the PI3K pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  25-OH-PPD inhibits hypertrophy on diabetic cardiomyopathy via the PI3k/Akt/GSK-3β signaling pathway. (Pubmed Central) -  Aug 9, 2020   
    The animals were divided into 5 groups as follows: Normal group (NG group), diabetic group, PPD treatment group, PPD/LY294002 group (inhibitor of PI3K/Akt) and PPD/LiCl group [inhibitor of glycogen synthase kinase (GSK) 3β]...In addition, PPD treatment significantly increased the expression levels of p-Akt and decreased the levels of phosphorylated GSK-3β compared with those of the DMCM group (P<0.05). The data demonstrated that the protective effects of 25-OH-PPD against DMCM may be attributed to the PI3k/Akt/GSK-3β signaling pathway, via the suppression of the α-SMA/VCAM axis and the downregulation of TGF-β1 and CTGF expression.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, tivantinib (ARQ 197) / Daiichi Sankyo, Kyowa Hakko Kirin, Merck (MSD)
    Journal:  Human umbilical cord MSC-derived hepatocyte growth factor enhances autophagy in AOPP-treated HK-2 cells. (Pubmed Central) -  Aug 9, 2020   
    Furthermore, the effects of tivantinib were reversed by Ly294002. In conclusion, the present study revealed that hUC-MSCs partially reversed AOPP-mediated inhibition of autophagy in HK-2 cells via secretion of HGF, indicating that hUC-MSCs may serve as a potential therapy for preventing the progression of CKD.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  Lycopene attenuates high glucose-mediated apoptosis in MPC5 podocytes by promoting autophagy via the PI3K/AKT signaling pathway. (Pubmed Central) -  Aug 9, 2020   
    To explore the effects of Lyc on the PI3K/AKT signaling pathway and autophagy, LY294002 (LY) and 3-methyladenine (3-MA) were used as PI3K and autophagy inhibitors, respectively...In addition, the effects of Lyc on HG-mediated MPC5 podocyte apoptosis were alleviated by 3-MA. Therefore, the present study suggested that Lyc may protect against HG-induced MPC5 podocyte apoptosis by promoting autophagy activity via activation of the PI3K/AKT signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Crixivan (indinavir sulfate) / Merck (MSD)
    Journal:  Fibroblast growth factor-21 potentiates glucose transport in skeletal muscle fibers. (Pubmed Central) -  Aug 7, 2020   
    The use of PI3K inhibitors such as Wortmannin (100 nM) and LY294002 (50 µM) completely prevented the FGF21-dependent glucose uptake...FGF21 at low concentrations potentiated the effect of insulin on glucose uptake but at high concentrations, completely inhibited the uptake in the presence of insulin. These results suggest that FGF21 regulates glucose uptake by a mechanism mediated by GLUT4 and dependent on atypical PKC-ζ- in skeletal muscle.
  • ||||||||||  everolimus / Generic mfg., pimasertib (AS703026) / EMD Serono, Sanofi
    Journal:  mTOR inhibitor everolimus reduces invasiveness of melanoma cells. (Pubmed Central) -  Aug 5, 2020   
    Slightly less profound reduction of invasiveness was obtained for the combinations of an mTOR inhibitor-everolimus with ERK1/2 inhibitor-U126 or MEK inhibitor-AS-703026 and in the case of MMPs activity decrease for PI3 K inhibitor-LY294002 and AKT inhibitor-MK-2206. The simultaneous use of everolimus or another new generation rapalog with selected inhibitors of crucial signaling kinases seems to be a promising concept in cancer treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  NAD precursors protect corneal endothelial cells from UVB-induced apoptosis. (Pubmed Central) -  Aug 5, 2020   
    In addition, the capacity of NIC to protect CECs was fully reversed in the presence of the AKT inhibitor LY294002. Therefore, we conclude that NAD precursors can effectively prevent the apoptosis of the corneal endothelium through reactivating AKT signaling; this represents a potential therapeutic approach for preventing UVB-induced corneal damage.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  MST4 inhibits human hepatocellular carcinoma cell proliferation and induces cell cycle arrest via suppression of PI3K/AKT pathway. (Pubmed Central) -  Aug 4, 2020   
    Importantly, mechanistic investigations suggested that dnMST4 significantly elevated the phosphorylation levels of key members of PI3K/AKT pathway, and the selective PI3K inhibitor LY294002 can reverse the proliferation-promoting effect of dnMST4. Overall, our results provide a new insight into the clinical significance, functions and molecular mechanism of MST4 in HCC, suggesting that MST4 might have a potential therapeutic value in the HCC clinical treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Role of IGFBP1 in the senescence of vascular endothelial cells and severity of aging‑related coronary atherosclerosis. (Pubmed Central) -  Jul 29, 2020   
    In cultured HCAECs, IGFBP1 was shown to protect ECs against passage‑ or H2O2‑induced senescence, and these protective effects of IGFBP1 may be partially reversed by LY294002, a known Akt signaling inhibitor. Therefore, the results of the present study suggested that, as a downstream protein of Jagged1, IGFBP1 was correlated with the severity of coronary atherosclerosis in aging patients, and the increase of circulating IGFBP1 levels with aging may be an adaptive response to counter HCAEC senescence through Akt signaling.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  MicroRNA-221 Modulates Airway Remodeling via the PI3K/AKT Pathway in OVA-Induced Chronic Murine Asthma. (Pubmed Central) -  Jul 28, 2020   
    A PI3K/AKT-inhibitor (LY294002) was used to confirm the role of the pathway in ASMCs...Bioinformatics analysis and western blot analysis confirmed that the PI3K-AKT pathway was involved in ECM deposition in ASMCs. miR-221 might play a crucial role in the mechanism of remodeling via the PI3K/AKT pathway in chronic asthma and it could be considered as a potential target for developing therapeutic strategies.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Prolonged high-glucose exposure decreased SREBP-1/FASN/ACC in Schwann cells of diabetic mice via blocking PI3K/Akt pathway. (Pubmed Central) -  Jul 25, 2020   
    LY294002 suppressed Akt activation followed by the decreased SREBP-1, FASN, ACC, triglyceride, and cholesterol...The knockdown of SREBP-1 by shRNA prevented insulin-induced enhanced FASN, ACC mRNA expression, triglyceride, and cholesterol in high-glucose-treated RSC96 cells. In conclusion, prolonged high-glucose exposure inhibits the SREBP-1/FASN/ACC expression in the Schwann cells of DPN via the blockage of the PI3K/Akt signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega
    Journal:  Sal B targets TAZ to facilitate osteogenesis and reduce adipogenesis through MEK-ERK pathway. (Pubmed Central) -  Jul 21, 2020   
    Moreover, Sal B increased the p-ERK/ERK ratio to regulate the TAZ expression as well as the cell differentiation. In summary, this study suggests for the first time that Sal B targets TAZ to facilitate osteogenesis and reduce adipogenesis by activating MEK-ERK signalling pathway, which provides evidence for Sal B to be used as a potential therapeutic agent for the management of bone diseases.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega
    Journal:  p22phox promotes Ang-II-induced vascular smooth muscle cell phenotypic switch by regulating KLF4 expression. (Pubmed Central) -  Jul 21, 2020   
    Furthermore, HO treatment effectively enhanced the phosphorylation of AKT, ERK1/2 and the expression of KLF4, whereas LY294002 (a specific inhibitor of PI3K), U0126 (a specific inhibitor of ERK1/2) significantly attenuated the H2O2-induced up-regulation of KLF4. In conclusion, these results demonstrated that p22phox promotes Ang-II-induced VSMC phenotypic switch via the HO-ERK1/2/AKT-KLF4 signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, PARP Biomarker, PD(L)-1 Biomarker, IO biomarker:  α-Cyperone inhibits the proliferation of human cervical cancer HeLa cells via ROS-mediated PI3K/Akt/mTOR signaling pathway. (Pubmed Central) -  Jul 21, 2020   
    Interestingly, the expression of PD-L1 was attenuated by both α-Cyperone and LY294002, while the supplement of IGF-1 rescued the low expression of PD-L1. In conclusion, our results reveal that the inhibitory effect of α-Cyperone on HeLa cell growth is triggered via the ROS-mediated PI3K/Akt/mTOR signaling pathway and closely related to a decline in the PD-L1 expression.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Elevated S100A4 in asthmatics and an allergen-induced mouse asthma model. (Pubmed Central) -  Jul 18, 2020   
    We further showed that LY294002, a specific inhibitor of PI3K, markedly decreased S100A4 expression in lung and S100A4 secretion in BALF in asthmatic mice. In conclusion, these data demonstrated that S100A4 may be involved in the pathogenesis of airway inflammation in asthma.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Biomarker, Journal:  LETM1 is a potential biomarker that predicts poor prognosis in gastric adenocarcinoma. (Pubmed Central) -  Jul 18, 2020   
    Taken together, our results demonstrate that LETM1 regulates cell proliferation and promotes tumorigenicity of GA, and its overexpression is associated with the poor progression of GA. Therefore, LETM1 could serve as a potential prognostic biomarker and a therapeutic target for the better clinical management of GA.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  FAM3A protects chondrocytes against interleukin-1β-induced apoptosis through regulating PI3K/Akt/mTOR pathway. (Pubmed Central) -  Jul 16, 2020   
    Moreover, mechanistically, FAM3A activated PI3K/Akt/mTOR pathway in IL-1β-treated chondrocytes, and blockade of PI3K/Akt/mTOR pathway with specific inhibitors, wortmannin and LY294002, diminished FAM3A effect on IL-1β-induced chondrocyte apoptosis, hence demonstrating that FAM3A attenuates IL-1β-induced chondrocyte apoptosis through activating the pro-survival PI3K/Akt/mTOR pathway. In conclusion, our study may identify FAM3A as a potential regulator of chondrocyte apoptosis involved in OA pathogenesis.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, dactolisib (RTB101) / resTORbio
    [VIRTUAL] PI3K inhibitor add-on strategy improve glucocorticoid insensitivity in severe asthma (Pre-congress content) -  Jul 15, 2020 - Abstract #ERS2020ERS_2164;    
    The ability of compounds including PI3K inhibitors (BEZ235 and LY294002) to ameliorate GC insensitivity in severe asthma was evaluated. This study demonstrates that PI3K inhibitors ameliorate GC insensitivity in severe asthma by restoring HDAC2 activity and inhibiting the phosphorylation of nuclear signaling transcription factors.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Bay11-7082 / InvivoGen
    Journal:  RPS15A promotes gastric cancer progression via activation of the Akt/IKK-β/NF-κB signalling pathway. (Pubmed Central) -  Jul 8, 2020   
    Collectively, our findings suggest that RPS15A activates the NF-κB pathway through Akt/IKK-β signalling axis, and consequently promotes EMT and GC metastasis. This newly identified RPS15A/Akt/IKK-β/NF-κB signalling pathway may be a potential therapeutic target to prevent GC progression.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    [VIRTUAL] Co-Cultured BM-MSCs Enhance Phagocytosis and Down-Regulate Autophagy of Macrophages Via PI3K/Akt Signaling Pathway (ATS 2020 Virtual) -  Jul 6, 2020 - Abstract #ATSI2020ATS-I_5972;    
    Vise versa, pre-conditioned with LY294002, the inhibitor of PI3K, macrophages reversely expressed those biomarks in this co-culture systems, strongly suggesting the crucial role of PI3K/Akt signaling pathway underlying the modulations of BM-MSCs on macrophages. This work also further highlights the importance of BM-MSCs and its beneficial modulations on macrophages under OGD/R circumstance.
  • ||||||||||  [VIRTUAL] Non-Genomic Effects of Glucocorticoids Differentially Modulate Glucocorticoid Receptor Site-Specific Phosphorylation (ATS 2020 Virtual) -  Jul 6, 2020 - Abstract #ATSI2020ATS-I_3745;    
    The role of protein synthesis as well as GR was also examined using cycloheximide and RU486, respectively...While SB203580 and LY294002 had little effect on CB-induced pGR-ser226, PD98059 and SP600125 dramatically reduced pGR-ser226...Conclusion Together, our findings show that the non-genomic effects of GC i) differentially affect GR phosphorylation by upregulating pGR-ser226, but not pGR-ser211, in a manner that is GR-independent but ERK/JNK dependent and ii) rapidly activate MAPK pathways. Further studies are still needed to determine the role of GR-independent early events such as nonspecific interactions with the cell membrane in regulating later GC genomic activities.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  LncRNA TDRG1 Promotes Proliferation, Invasion and Epithelial-Mesenchymal Transformation of Osteosarcoma Through PI3K/AKT Signal Pathway. (Pubmed Central) -  Jul 3, 2020   
    L740Y-P (activator of PI3K/AKT pathway) and LY294002 (inhibitor of PI3k/AKT pathway) were used to interfere with PI3k/Akt signaling pathway in osteosarcoma cells...TDRG1 is highly expressed in osteosarcoma tissue. Silencing the expression of osteosarcoma can inhibit the proliferation, invasion, migration and EMT of osteosarcoma cells by inhibiting PI3K/AKT signaling pathway, which may be a new target for diagnosis and treatment of osteosarcoma.