LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly, U0126 / Promega, clopidogrel / Generic mfg.
    Journal:  LongShengZhi Capsule reduces carrageenan-induced thrombosis by reducing activation of platelets and endothelial cells. (Pubmed Central) -  Mar 24, 2020   
    We also compared the therapeutic effects of LSZ and clopidogrel on formed thrombi...LSZ also reduced adhesion molecules or tissue factor but activated tissue factor pathway inhibitor expression in HUVECs. Taken together, our study demonstrates the antithrombotic properties of LSZ by reducing activation of platelets and endothelial cells, and suggests its potential application in clinics.
  • ||||||||||  irinotecan / Generic mfg.
    Journal:  Decreasing Arl4c expression by inhibition of AKT signal in human lung adenocarcinoma cells. (Pubmed Central) -  Mar 24, 2020   
    The combination of atorvastatin and resveratrol has the potential of accelerating re-endothelialization after stent implantation, reducing the risk of thrombosis and improving the safety of DESs. Here, we highlighted the AKT pathway as an important regulatory pathway for Arl4c expression in lung cancer cells and identified HCPT as a promising drug for lung adenocarcinoma treatment that functioned by targeting Arl4c expression.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Integrin β1 in Adipose-Derived Stem Cells Accelerates Wound Healing via Activating PI3K/AKT Pathway. (Pubmed Central) -  Mar 23, 2020   
    Here, we highlighted the AKT pathway as an important regulatory pathway for Arl4c expression in lung cancer cells and identified HCPT as a promising drug for lung adenocarcinoma treatment that functioned by targeting Arl4c expression. Integrin β1 can promote the migration and endothelial-like differentiation of ADSCs by activating PI3K/AKT pathway and then enhance the function of ADSCs in promoting wound healing.
  • ||||||||||  medroxyprogesterone injection / Generic mfg.
    Biomarker, Journal:  CRISPR/Cas9-mediated gene knockout of ARID1A promotes primary progesterone resistance by downregulating progesterone receptor B in endometrial cancer cells. (Pubmed Central) -  Mar 22, 2020   
    Medroxyprogesterone (MPA) is used for the conservative treatment of endometrial cancer...The sensitivity of the parental Ishikawa, Ishikawa-PR, and ARID1A-deficient cells to MPA and/or LY294002 was determined using the Cell Counting Kit-8 (CCK-8) assay and flow cytometry analysis...Akt inhibition cannot rescue PRB or sensitize to MPA in ARID1A knockout cells. These findings suggest that ARID1A may be act as a reliable biomarker to predict the response for the combination of AKT inhibitor and MPA treatment.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Suppression of SEMA6C promotes preantral follicles atresia with decreased cell junctions in mice ovaries. (Pubmed Central) -  Mar 20, 2020   
    And the LY294002, a PI3K inhibitor, could reverse the effect of low SEMA6C expression on cell junctions in preantral follicles. Our findings revealed that Sema6c was involved in follicle development, and the suppression of SEMA6C led to cell junction defection by activating the PI3K/AKT pathway, which might also provide valuable information for understanding premature ovarian failure and ovarian aging.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, etoposide IV / Generic mfg.
    Journal:  JmjC domain-containing protein 8 (JMJD8) represses Ku70/Ku80 expression via attenuating AKT/NF-κB/COX-2 signaling. (Pubmed Central) -  Mar 18, 2020   
    In conclusion, our research provided data to establish the role of JMJD8 in regulating tumor cell proliferation and their sensitivity to ionizing irradiation or chemo-therapy drug, and the AKT/NF-κB/COX-2 signaling mediated expression of Ku70/Ku80 was involved. The results of this research indicated that JMJD8 is a potential target for enhancing the efficacy of tumor radio- and chemo-therapies.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  The role of PI3K-mediated AMPA receptor changes in post-conditioning of propofol in brain protection. (Pubmed Central) -  Mar 18, 2020   
    The short-term neuroprotective effect was contributed by enhanced GluR2 subunits trafficking to membrane and postsynaptic membranes of neurons, as well as down-regulated the expression of pGluR2 in damaged hippocampus. Finally, the above-mentioned protective mechanism might be contributed by increased combination of PI3K to AMPAR GluR2 subunit, thus maintained the expression and activation of AMPAR GluR2 in the ipsilateral hippocampus.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Co-Cultured BM-MSCs Enhance Phagocytosis and Down-Regulate Autophagy of Macrophages Via PI3K/Akt Signaling Pathway (PENNSYLVANIA CONVENTION CENTER, Hall D-E (200 Level), Area D) -  Mar 15, 2020 - Abstract #ATS2020ATS_8597;    
    We found that the modulations of BM-MSCs on macrophages were through enhancingphagocytosis, reducing apoptosis, down-regulating autophagy, decreasing expressions of inflammatory mediators and promoting M1 polarization,viaPI3K/Akt signalingpathway.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.
  • ||||||||||  Non-Genomic Effects of Glucocorticoids Differentially Modulate Glucocorticoid Receptor Site-Specific Phosphorylation (PENNSYLVANIA CONVENTION CENTER, Hall D-E (200 Level), Area C) -  Mar 15, 2020 - Abstract #ATS2020ATS_6138;    
    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.
  • ||||||||||  Decadron (dexamethasone) / Merck (MSD)
    Corticosteroids Phosphorylate Glucocorticoid Receptor at the Newly Described Residue Serine 134 in Airway Smooth Muscle Cells (PENNSYLVANIA CONVENTION CENTER, Room 126 A-B (100 Level)) -  Mar 15, 2020 - Abstract #ATS2020ATS_3500;    
    Conclusion Collectively, we demonstrated for the first time in primary cells that GC phosphorylates GR at ser134 residue by involving non-genomic mechanisms that are mGR/JNK-dependent. Further studies are still needed to determine the role of pGRser134 in i) mediating non-genomic effects of GC and in regulating later GC genomic activities and ii) GR signaling and GC actions in cells derived from healthy and asthmatic patients.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO Biomarker:  Chlamydia muridarum infection induces CD4+ T cells apoptosis via PI3K/AKT signal pathway. (Pubmed Central) -  Mar 13, 2020   
    The present study demonstrated that phosphatidylinositol 3-kinase (PI3K) p110δ mRNA and phosphorylation of protein kinase B (p-AKT) level were significantly increased in lung cells and spleen cells at day 3 and day 7 post-infection, p-AKT level was inhibited when adding PI3K inhibitor LY294002...The related apoptosis proteins Bcl-2 and Mcl-1 uneven expression levels were induced in CD4+ T cells by Cm infection. These findings provided in vivo and in vitro evidence that Cm infection induces CD4+ T cells apoptosis possibly via PI3K/AKT signal pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Shenfu Injection Promotes Vasodilation by Enhancing eNOS Activity Through the PI3K/Akt Signaling Pathway In Vitro. (Pubmed Central) -  Mar 13, 2020   
    Furthermore, it promoted the expression of total eNOS and the phosphorylation of eNOS at serine (Ser) 1177 but inhibited the phosphorylation at threonine (Thr) 495, which was significantly reversed by PI3K-specific inhibitor LY294002. In conclusion, our study showed the vasodilation effect of SFI in thoracic aorta is mediated entirely by enhancing eNOS activity through the PI3K/Akt signaling pathway, providing novel knowledge on the effect of SFI on shock and HF for future clinical applications.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, gefitinib / Generic mfg., PD98059 / Wayne State University
    Journal:  EGF receptor stimulation shifts breast cancer cell glucose metabolism toward glycolytic flux through PI3 kinase signaling. (Pubmed Central) -  Mar 10, 2020   
    Blocking EGFR activation with BIBX1382 or gefitinib completely abolished both FDG uptake and proliferation effects...Increased cell proliferation by EGFR stimulation was completely abolished by MAPK inhibition with PD98059 or by PI3K inhibition with LY294002...These findings suggest that the association between breast tumor EGFR expression and high FDG uptake might be contributed by stimulation of the PI3K pathway downstream of EGFR activation. This was in contrast to EGFR-mediated cell proliferation that required MAPK as well as PI3K signaling.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, dalfampridine / Generic mfg.
    Preclinical, Journal:  Blockade of voltage-gated potassium channels ameliorates diabetes-associated cognitive dysfunction in vivo and in vitro. (Pubmed Central) -  Mar 4, 2020   
    Additionally, the PI3K inhibitor LY294002 partially abolished the effects of TEA and 4-AP. These findings indicate that the blockade of Kv channels by TEA and 4-AP ameliorates the diabetes-associated cognitive dysfunction via PI3K/Akt pathway, suggesting that targeting Kv channels could be a promising strategy for the treatments of cognitive impairments in diabetes.
  • ||||||||||  tivantinib (ARQ 197) / Daiichi Sankyo, Kyowa Hakko Kirin, Merck (MSD)
    Journal:  Tivantinib Hampers the Proliferation of Glioblastoma Cells via PI3K/Akt/Mammalian Target of Rapamycin (mTOR) Signaling. (Pubmed Central) -  Mar 3, 2020   
    Tivantinib (1 μmol/L) in combination with PI3K inhibitor LY294002 (0.5 μmol/L) and mTOR inhibitor rapamycin (0.1 nmol/L) largely inhibited the proliferation of glioblastoma cells. CONCLUSIONS c-MET inhibitor tivantinib blocks PIKE/Akt/mTOR signaling and hampers the proliferation of glioblastoma cells, which endows the drug a therapeutic effect.
  • ||||||||||  metformin / Generic mfg., quercetin (LY294002) / Eli Lilly
    Journal:  Evaluation of Angiogenesis Process After Metformin and LY294002 Treatment in Mammary Tumor. (Pubmed Central) -  Mar 2, 2020   
    CONCLUSIONS c-MET inhibitor tivantinib blocks PIKE/Akt/mTOR signaling and hampers the proliferation of glioblastoma cells, which endows the drug a therapeutic effect. Our results demonstrate the effectiveness of metformin and LY294002 in controlling the angiogenesis process in mammary tumors by VEGF and HIF-1, the most important angiogenic markers.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Aberrant IGF1-PI3K/AKT/MTOR signaling pathway regulates the local immunity of oral lichen planus. (Pubmed Central) -  Mar 2, 2020   
    Our results demonstrate the effectiveness of metformin and LY294002 in controlling the angiogenesis process in mammary tumors by VEGF and HIF-1, the most important angiogenic markers. The aberrant IGF1-PI3K/AKT/MTOR signaling may participate in the immunoregulatory mechanism of OLP, via regulation on the crosstalk between T cells and keratinocytes, as well as imbalanced cytokine networks.
  • ||||||||||  Jakafi oral (ruxolitinib) / Novartis, Incyte, Xeljanz (tofacitinib) / Pfizer
    Biomarker, Journal, PD(L)-1 Biomarker, IO Biomarker:  Interferon-γ upregulates Δ42PD1 expression on human monocytes via the PI3K/AKT pathway. (Pubmed Central) -  Mar 2, 2020   
    We demonstrated that IFN-γ increases Δ42PD1 expression on human monocytes via activating the PI3K/AKT signaling pathway downstream of JAKs, and that the PD-1 Δ/F ratio is a potential biomarker to predict the functional state of monocytes. Notably, we revealed the Δ42PD1 play a role in T-cell regulation, providing a novel potential approach to manipulate adaptive immune response.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  The protective effects of Ghrelin/GHSR on hippocampal neurogenesis in CUMS mice. (Pubmed Central) -  Mar 2, 2020   
    Furthermore, the in vivo data displayed that LY294002 (50 nmol, i.c.v.) can significantly block the antidepressant-like action of exogenous ghrelin treatment. All these results suggest that ghrelin/GHSR signaling maintains the integrity of hippocampus and has an inherent neuroprotective effect whether facing stress or not.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Contraction dynamics of dental pulp cell rod microtissues. (Pubmed Central) -  Mar 2, 2020   
    All these results suggest that ghrelin/GHSR signaling maintains the integrity of hippocampus and has an inherent neuroprotective effect whether facing stress or not. The field of regenerative endodontology will benefit from our findings as it can be applied as a novel platform to test the impact of pharmacological agents, biomaterials, and regenerative approaches including bioprinting.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, dactolisib (RTB101) / resTORbio
    Journal:  PI3K inhibitor treatment ameliorates the glucocorticoid insensitivity of PBMCs in severe asthma. (Pubmed Central) -  Mar 1, 2020   
    This analysis predicted several kinds of small-molecule compounds to treat JDM. 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
    Akt-dependent Regulation of Nitric Oxide and Inflammation in Airway Cells (Convention Center, 200 Level, Hall D) -  Mar 1, 2020 - Abstract #AAAAI2020AAAAI_1597;    
    Additionally, treatment with SC79 reversed TNF-α induced IL-6 and IL-8 in airway cells. Future work will be directed toward testing the downstream mechanisms of eNOS/NO in response to SC79 in patient-derived primary cells.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, dactinomycin / Generic mfg.
    Journal:  Zinc induces iron uptake and DMT1 expression in Caco-2 cells via a PI3K/IRP2 dependent mechanism. (Pubmed Central) -  Feb 26, 2020   
    In agreement with these findings zinc treatment stabilized DMT1 mRNA levels in actinomycin-D treated cells. Based on these findings, we conclude that zinc-induced iron absorption involves elevation of DMT1 expression via stabilization of its mRNA, via a PI3K/IRP2-dependent mechanism.
  • ||||||||||  glibenclamide / Generic mfg.
    Preclinical, Journal:  Marjoram Relaxes Rat Thoracic Aorta Via a PI3-K/eNOS/cGMP Pathway. (Pubmed Central) -  Feb 26, 2020   
    Blockers of ATP-sensitive or Ca2+-activated potassium channels such as glibenclamide or tetraethylamonium (TEA), respectively, did not significantly affect OME-induced relaxation...Our findings further support the medicinal value of marjoram and provide a basis for its beneficial intake. Although consuming marjoram may have an antihypertensive effect, further studies are needed to better determine its effects in different vascular beds.