LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Pentraxin 3 promotes the osteoblastic differentiation of MC3T3-E1 cells through the PI3K/Akt signaling pathway. (Pubmed Central) -  Mar 31, 2021   
    Mechanistically, we show that the action of PTX3 requires the activation of PI3K and Akt, and deactivation of PI3K by its inhibitor LY294002 weakens the PTX3-mediated induction of osteoblast signature genes, ALP, and matrix mineralization. This study revealed a new role played by PTX3 and suggest a potential mechanism governing the osteoblastic differentiation of MC3T3-E1 cells.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  TREM2 ameliorates neuroinflammatory response and cognitive impairment via PI3K/AKT/FoxO3a signaling pathway in Alzheimer's disease mice. (Pubmed Central) -  Mar 30, 2021   
    This phenomenon can be abolished by applying the PI3K inhibitor LY294002, suggesting FoxO3a not only participates in TREM2-induced anti-inflammation response, but is also involved in regulating the phenotype of microglia. Taken together, our results show that the protective functions of TREM2, both in inflammatory response and cognitive impairment as well as in the decrease of M1 phenotype microglia, are related to PI3K/AKT/FoxO3a signaling pathway in AD mice.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Histone Deacetylase SIRT1 Mediates C5b-9-Induced Cell Cycle in Oligodendrocytes. (Pubmed Central) -  Mar 26, 2021   
    To investigate the signaling pathway activated by C5b-9 and required for SIRT1 expression, we pretreated OLGs with a c-jun antisense oligonucleotide, a phosphoinositide 3-kinase (PI3K) inhibitor (LY294002), and a protein kinase C (PKC) inhibitor (H7)...Inhibition of SIRT1 with sirtinol also abolished C5b-9-induced DNA synthesis. Taken together, these data show that induction of SIRT1 expression by C5b-9 is required for cell cycle activation and is mediated through multiple signaling pathways.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO biomarker:  Protective effects of peptide FK18 against neuro-excitotoxicity in SH-SY5Y cells. (Pubmed Central) -  Mar 23, 2021   
    FK18 also increased the Bcl-2/Bax ratio and decreased the level of cleaved-caspase-3 in SY5Y cells, which was reversed by the Akt pathway inhibitor LY294002, but not by the Erk pathway inhibitor U0126. The findings of the present study suggested that FK18 may be a promising therapeutic agent for the inhibition of neuronal cell death in multiple neurological diseases involving excitotoxicity.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, AZD9056 / AstraZeneca
    Journal:  PI3K/Akt/GSK-3β signal pathway is involved in P2X7 receptor-induced proliferation and EMT of colorectal cancer cells. (Pubmed Central) -  Mar 20, 2021   
    P13/Akt pathway inhibitor LY294002 inhibited the proliferation of CRC cells, and the P13/Akt signaling was required for BzATP induced the proliferation of CRC cells. Our conclusion is that P2X7R mediated the PI3K/Akt/GSK-3beta signaling to promote the proliferation and EMT of CRC, indicating that P2X7R may be used as a potential therapeutic target for CRC.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  MUC15 inhibits cancer metastasis via PI3K/AKT signaling in renal cell carcinoma. (Pubmed Central) -  Mar 19, 2021   
    Interruption of the AKT pathway with the specific inhibitor LY294002 could reverse the expression of MMPs. Therefore, our study clarify the novel function of MUC15 in RCC, which may provide a new sight to diagnose and prevent RCC metastasis.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  MicroRNA-185 inhibits the proliferation and migration of HaCaT keratinocytes by targeting peroxisome proliferator-activated receptor β. (Pubmed Central) -  Mar 19, 2021   
    Furthermore, PI3K inhibitor LY294002 inhibited activation of the PI3K/AKT signaling pathway and decreased the proliferation and migration of HaCaT keratinocytes...In conclusion, the results of the present study demonstrated that miR-185 suppressed activation of the PI3K/AKT signaling pathway via targeting PPARβ, thereby regulating proliferation and migration in HaCaT keratinocytes. The present study provided a novel theoretical basis for the use of miR-185 as a target in wound repair.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Piperine protects against myocardial ischemia/reperfusion injury by activating the PI3K/AKT signaling pathway. (Pubmed Central) -  Mar 19, 2021   
    Mechanistic studies concluded that the apoptosis-inhibitory contributions and cardio-favorable effects of PIP were caused partly by the activation of the PI3K/AKT signaling pathway, which was verified by LY294002 administration. To conclude, PIP can reduce ERS-induced apoptosis by activating the PI3K/AKT signaling pathway during the process of H/R injury, which could be a potential therapeutic target for the treatment of myocardial ischemia/reperfusion injury.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
    Preclinical, Journal:  Expression of canonical transient receptor potential channels in U-2 OS and MNNG-HOS osteosarcoma cell lines. (Pubmed Central) -  Mar 19, 2021   
    The data shows in principle, and consistent with the literature, that the signaling pathways examined can regulate the expression of TRPCs at the mRNA level. Therefore, direct and signaling pathway-specific pharmacological targeting of TRPC subtypes may represent an option for improving the treatment of osteosarcoma.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Apelin-13/APJ system delays intervertebral disc degeneration by activating the PI3K/AKT signaling pathway. (Pubmed Central) -  Mar 16, 2021   
    In summary, we concluded that ILF3-AS1 provides protection against hypoxia-induced injury via the PI3K/Akt pathway, which may provide clues for the treatment of patients with MI. Apelin-13/APJ system activates PI3K/AKT signaling pathway activity, reduces the degradation of nucleus pulposus extracellular matrix, promotes proliferation, and reduces the level of apoptosis and inflammation, thus delaying the degeneration of the intervertebral disc.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO biomarker:  Mangiferin attenuates IL-1β-induced chondrocytes apoptosis. (Pubmed Central) -  Mar 16, 2021   
    Apelin-13/APJ system activates PI3K/AKT signaling pathway activity, reduces the degradation of nucleus pulposus extracellular matrix, promotes proliferation, and reduces the level of apoptosis and inflammation, thus delaying the degeneration of the intervertebral disc. Mangiferin could attenuate IL-1β-induced apoptosis of the mice chondrocytes, which is mediated by the activation of PI3K/Akt signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    [VIRTUAL] Inflammation-Induced Pericyte Dysfunction Is Abrogated by Interfering with the CXCL12/CXCR4 Signaling Pathway () -  Mar 14, 2021 - Abstract #ATS2021ATS_3414;    
    LIT9-27 is able to reverse CXCL12-induced pericyte migration monocyte transmigration back to control levels. Notably, LIT-927 appeared to be equipotent to MAPK inhibitors in the suppression of CXCL12-induced pericyte migration, indicating that LIT927 is an effective therapeutic alternative to MAPK inhibitors in the treatment of inflammation-induced vascular dysfunction.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  PENK inhibits osteosarcoma cell migration by activating the PI3K/Akt signaling pathway. (Pubmed Central) -  Mar 13, 2021   
    Notably, LIT-927 appeared to be equipotent to MAPK inhibitors in the suppression of CXCL12-induced pericyte migration, indicating that LIT927 is an effective therapeutic alternative to MAPK inhibitors in the treatment of inflammation-induced vascular dysfunction. PENK inhibits OS cell migration by activating the PI3K/Akt signaling pathway.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  High-Fat Diet-Related Obesity Promotes Urethane-Induced Lung Tumorigenesis in C57BL/6J Mice. (Pubmed Central) -  Mar 13, 2021   
    These effects were significantly attenuated when PI3K or mTOR were inhibited by LY294002 or rapamycin, respectively. These results suggested that HFD-induced obesity could promote the development of lung tumorigenesis in C57BL/6J mice, and leptin-mediated activation of the PI3K/Akt/mTOR/STAT3 pathway was likely involved in this mechanism.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    [VIRTUAL] RCC2 promotes glioblastoma through regulation of G2-M progression () -  Mar 11, 2021 - Abstract #AACR2021AACR_1137;    
    Additionally, the connectivity map (C-map) analysis was conducted and identified LY294002 and cephaeline as promising inhibitors for RCC2-associated gene signatures...We provided evidence that RCC2 exerts a positive effect on G2-M progression. These findings may shed light on anti-RCC2 targeted therapy in GBM treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Novel antiproliferative agents bearing morpholinopyrimidine scaffold as PI3K inhibitors and apoptosis inducers; design, synthesis and molecular docking. (Pubmed Central) -  Mar 9, 2021   
    The IC values were very promising: compound [6e = 11.73 (α), 6.09 (β), 11.18 (δ)], compound [6g = 8.43 (α), 15.84 (β), 30.62 (δ)], and compound [6l = 13.98 (α), 7.22 (β), 10.94 (δ)], compared to the reference compound LY294002 = 6.28 (α), 4.51 (β), 4.60 (δ) uM, respectively...Finally, docking study was performed to analyze the interactive mode of these derivatives in PI3Kα ATP-binding site. These outcomes proved that compounds 6e, 6g, and 6l are potential leads for further optimization as antileukemic agents.
  • ||||||||||  Victoza (liraglutide) / Novo Nordisk
    Journal:  Liraglutide Protects Nucleus Pulposus Cells Against High-Glucose Induced Apoptosis by Activating PI3K/Akt/ mTOR/Caspase-3 and PI3K/Akt/GSK3β/Caspase-3 Signaling Pathways. (Pubmed Central) -  Mar 9, 2021   
    The human NPCs were incubated with 100 nM liraglutide alone or in combination with LY294002 (PI3K inhibitor), rapamycin (mTOR inhibitor), and SB216763 (GSK3β inhibitor) in a high glucose culture for 48 h. The four groups were assessed further for apoptosis and genes expressions...Further assessments revealed that activation of mTOR and GSK3β was almost completely inhibited by rapamycin and SB216763, respectively, which significantly increased the caspase-3 levels. Liraglutide could protect NPCs against high glucose-induced apoptosis by activating the PI3K/AKT/mTOR/caspase-3 and PI3K/AKT/GSK3β/caspase-3 signaling pathways.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  8-prenylgenistein exerts osteogenic effects via ER α and Wnt-dependent signaling pathway. (Pubmed Central) -  Mar 6, 2021   
    Furthermore, the increase in ALP activity, LRP5 and phospho-Akt/Akt expression by 8PG and genistein were abolished by co-treatment with LY294002 (10 M, a PI3K pathway inhibitor). Collectively, our results suggested that the osteogenic activities of 8PG was mediated by GSK-3β phosphorylation through the induction of Wnt/β-catenin and ERα-associated PI3K/Akt signaling.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, PARP Biomarker, IO biomarker:  CNOT7 modulates biological functions of ovarian cancer cells via AKT signaling pathway. (Pubmed Central) -  Mar 6, 2021   
    Finally, activation of the PI3K/Akt pathway inhibits the Hippo pathway, resulting in nuclear YAP accumulation and accelerating MC proliferation and DN formation. CNOT7 has a carcinogenic effect in OC, and the carcinogenic effect may be achieved via the AKT signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Role of PI3-Kinase in Angiotensin II-Induced Cardiac Hypertrophy: Class I Versus Class III. (Pubmed Central) -  Mar 6, 2021   
    Ang II-induced autophagic increases were potentiated by inhibition of PI3KC1 with LY294002, but were impaired by inhibition of PI3KC3 with 3-methyladenine (3-MA)...Activation of PI3KC1 impairs autophagy activity, leading to accumulation of mitochondrial ROS, and, hence, cardiac hypertrophy. In contrast, activation of PI3KC3 improves autophagy activity, thereby reducing mitochondrial ROS and leads to a protective effect on Ang II-induced cardiac hypertrophy.
  • ||||||||||  progesterone / Generic mfg.
    Preclinical, Journal:  FSH Promotes Progesterone Synthesis by Enhancing Autophagy to Accelerate Lipid Droplet Degradation in Porcine Granulosa Cells. (Pubmed Central) -  Mar 6, 2021   
    Moreover, FSH treatment reduced the average number and size of LDs in porcine GCs, but these effects were eliminated by knocking down the key autophagy genes, ATG5 and BECLIN1; in addition, the effect of FSH on promoting progesterone secretion by the cells was also reduced significantly. Based on the above results, we concluded that FSH promoted progesterone production by enhancing autophagy through upregulation of Beclin1 via the PI3K/JNK/c-Jun pathway to accelerate LD degradation in porcine GCs, independent of the classical steroidogenic pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  The anti-UV properties of Saussurea involucrate Matsum. & Koidz. via regulating PI3K/Akt pathway in B16F10 cells. (Pubmed Central) -  Mar 5, 2021   
    These results suggest that the PI3K/Akt signaling pathway can promote proliferation and adipogenic differentiation of adipose stem cells, and that activation of this pathway by FGF2 may explain why hbASCs show greater proliferation and adipogenic differentiation than haASCs and htASCs. Our findings concluded that SIH protect melanoma cells from UV damages via activating PI3K/Akt signaling and which could provide scientific evidence for anti-UV pharmaceutical values of this herbal extract.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  κ‑opioid receptor agonist U50488H attenuates postoperative cognitive dysfunction of cardiopulmonary bypass rats through the PI3K/AKT/Nrf2/HO‑1 pathway. (Pubmed Central) -  Mar 3, 2021   
    Sprague‑Dawley rats were divided into the following groups: Sham operation (Sham group), CPB (CPB group), KOR agonist (U50488H) + CPB (U50488H group), CPB + U50488H + HO‑1 antagonist (ZnPP‑IX; ZnPP group) and CPB + U50488H + PI3K antagonist (LY294002; LY294002 group), with 10 rats in each group...In CPB rats treated with PI3K inhibitors, less Nrf2 was detected in the nucleus and HO‑1 and Trx‑1 expression levels were reduced in the nucleus. Therefore, U50488H, a KOR agonist, can activate Nrf2/HO‑1 via the PI3K/AKT pathway to improve cognitive function and reduce brain damage in CPB rats.