LY294002 / Eli Lilly 
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  • ||||||||||  glibenclamide / Generic mfg., verapamil / Generic mfg.
    Preclinical, Journal:  Gentiopicroside Produces Endothelium-Independent Vasodilation by Deactivating the PI3K/Akt/Rho-Kinase Pathway in Isolated Rat Thoracic Aorta. (Pubmed Central) -  Oct 1, 2021   
    Additionally, the vasorelaxation activity of GPS was attenuated upon pretreatment with LY294002 (PI3K/Akt inhibitor), Y27632 (Rho-kinase inhibitor), and verapamil (L-type Ca channel inhibitor). These findings demonstrate that GPS exhibits endothelium-independent vasorelaxant effects through inhibition of voltage-dependent, receptor-operated, and inositol triphosphate receptor (IPR)/ryanodine receptor- (RYR-) mediated Ca channels as well as the PI3K/Akt/Rho-kinase signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  2,6-Dimethoxy-1,4-benzoquinone increases skeletal muscle mass and performance by regulating AKT/mTOR signaling and mitochondrial function. (Pubmed Central) -  Oct 1, 2021   
    These findings demonstrate that GPS exhibits endothelium-independent vasorelaxant effects through inhibition of voltage-dependent, receptor-operated, and inositol triphosphate receptor (IPR)/ryanodine receptor- (RYR-) mediated Ca channels as well as the PI3K/Akt/Rho-kinase signaling pathway. Collectively, DMBQ was shown to increase skeletal muscle mass and performance by regulating the AKT/mTOR signaling pathway and enhancing mitochondrial function, which might be useful for the treatment and prevention of skeletal muscle atrophy.
  • ||||||||||  Cabometyx (cabozantinib tablet) / Takeda, Exelixis, Ipsen
    Journal, IO biomarker:  Activating CD137 Signaling Promotes Sprouting Angiogenesis via Increased VEGFA Secretion and the VEGFR2/Akt/eNOS Pathway. (Pubmed Central) -  Sep 29, 2021   
    Inhibition of VEGFR2 by siRNA or XL184 (cabozantinib) and inhibition of downstream signaling by LY294002 (inhibits AKT activation) and L-NAME (eNOS inhibitor) remarkably abolished proangiogenic effects of CD137 signaling both in vitro and ex vivo...In conclusion, activation of CD137 signaling promoted sprouting angiogenesis by increased VEGFA secretion and the VEGFR2/Akt/eNOS pathway. These findings provide a basis for stabilizing intraplaque angiogenesis through VEGFR2 intervatioin, as well as cancer treatment via combination of CD137 agonists and specific VEGFR2 inhibitors.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  CacyBP promotes the proliferation and invasion of non-small cell lung cancer (Pubmed Central) -  Sep 26, 2021   
    Compared with NC group, overexpression of CacyBP inhibited E-cadherin expression while promoted the expressions of N-cadherin, Snail1, Vimentin and p-Akt, which could be restored by LY294002. CacyBP may promote the proliferation and invasion of NSCLC cells by regulating Akt signal pathway.
  • ||||||||||  Opdivo (nivolumab) / Ono Pharma, BMS
    Journal, PD(L)-1 Biomarker, IO biomarker:  PD-L1 induces macrophage polarization toward the M2 phenotype via Erk/Akt/mTOR. (Pubmed Central) -  Sep 25, 2021   
    This study elucidates the role of PD-L1 in macrophage polarization and verifies the underlying mechanisms for the first time. Considering that aberrantly upregulated PD-L1 expression contributes to a wide variety of diseases, targeting PD-L1-mediated macrophage polarization is a prospective therapeutic strategy for both neoplastic and nonneoplastic diseases.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Methyltransferase-like 3 (METTL3) attenuates cardiomyocyte apoptosis with myocardial ischemia-reperfusion (I/R) injury through miR-25-3p and miR-873-5p. (Pubmed Central) -  Sep 24, 2021   
    Finally, the potential downstream mechanisms were investigated, and we expectedly found that METTL3 activated the PI3K/Akt pathway in H/R-treated cardiomyocytes through modulating miR-25-3p and miR-873-5p, and the PI3K/Akt pathway inhibitor (LY294002) abrogated the protective effects of METTL3 overexpression in cardiomyocytes with H/R treatment...Finally, the potential downstream mechanisms were investigated, and we expectedly found that METTL3 activated the PI3K/Akt pathway in H/R-treated cardiomyocytes through modulating miR-25-3p and miR-873-5p, and the PI3K/Akt pathway inhibitor (LY294002) abrogated the protective effects of METTL3 overexpression in cardiomyocytes with H/R treatment. Collectively, we concluded that METTL3 upregulated miR-25-3p and miR-873-5p to activate the PI3K/Akt pathway, resulting in the suppression of I/R injury.
  • ||||||||||  LY294002 / Eli Lilly
    [VIRTUAL] Omentin Reduces Angiotensin II-Induced Abdominal Aortic Aneurysm Formation in Apolipoprotein E Knockout Mice (ePosters) -  Sep 24, 2021 - Abstract #AHA2021AHA_6121;    
    Collectively, we concluded that METTL3 upregulated miR-25-3p and miR-873-5p to activate the PI3K/Akt pathway, resulting in the suppression of I/R injury. Our data indicate that omentin acts as an adipokine that can attenuate Ang II-induced development of AAA by reducing MMP9 and MMP2 expression through the integrin αVβ3/PI3-kinase/Akt signaling in the vascular wall.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Role of PI3K/AKT Signaling Pathway in Nucleus Pulposus Cells. (Pubmed Central) -  Sep 24, 2021   
    Nucleus pulposus (NP) cells were isolated from SD rat, and thereafter, passage three (P3) NP cells were divided into the following experimental groups: control, PI3K/AKT agonist IGF-1 (25 ng/ml, 50 ng/ml, and 100 ng/ml), and PI3K/AKT inhibitor LY294002 (5 μM, 10 μM, and 20 μM)...However, the activation of PI3K/AKT pathway partly prevented the NP cell from apoptosis and promoted their proliferation. Meanwhile, its activation also delayed the loss of extracellular matrix.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Scratch damaged tight junction through Akt/CLDN1 axis in atopic dermatitis. (Pubmed Central) -  Sep 23, 2021   
    PCB2 regulates the Nrf2/ARE signaling pathway by activating the P13K/Akt signaling pathway to protect mouse cerebral cortical neurons against oxidative injury induced by cypermethrin. The results reveal the underlying mechanism of tight junction damage promoted by scratching in the itch-scratch cycle of AD, and opens a new avenue to pruritus management in AD, through Akt antagonists.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, SP600125 / BMS
    Journal:  Cadmium induces CCL2 production in glioblastoma cells via activation of MAPK, PI3K, and PKC pathways. (Pubmed Central) -  Sep 19, 2021   
    Moreover, when cells were pretreated with Ro 32-0432 (an inhibitor of calcium-dependent PKC) and LY294002 (a PI3K inhibitor), this also resulted in a down-regulation of any Cd-induced CCL2 expression. Taken together, the results of this study allow for the conclusion to be made that CCL2 up-regulation in U-87 MG cells induced by Cd is mediated, in part, by an activation of MAPK, PI3K/Akt, and PKC pathways.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  MARCH5 restores endothelial cell function against ischaemic/hypoxia injury via Akt/eNOS pathway. (Pubmed Central) -  Sep 19, 2021   
    The protective effects mediated by MARCH5 overexpression on ECs could be inhibited by eNOS inhibitor L-NAME and Akt inhibitor LY294002. In conclusion, these results indicated that MARCH5 acts as a protective factor in ischaemia/hypoxia-induced ECs injury partially through Akt/eNOS pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Round Scad-Derived Octapeptide WCPFSRSF Confers Neuroprotection by Regulating Akt/Nrf2/NFκB Signaling. (Pubmed Central) -  Sep 19, 2021   
    Moreover, there is an interaction between the up-regulation of Nrf2 and the down-regulation of NFκB induced by the peptide, which was related to the generation of reactive oxygen species (ROS) and could be abolished by the Akt inhibitor LY294002...Moreover, WCPFSRSF could improve spatial memory impairment in sleep-deprived mice. Thus, this work provided evidence for WCPFSRSF as a potential candidate against neurotoxicity and memory deficits.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  S-oxiracetam Facilitates Cognitive Restoration after Ischemic Stroke by Activating α7nAChR and the PI3K-Mediated Pathway. (Pubmed Central) -  Sep 16, 2021   
    Furthermore, we found that methyllycaconitine, the antagonist of α7 nicotinic acetylcholine receptor (α7nAChR), and LY294002, the inhibitor of phosphoinositide 3-kinase (PI3K), were able to block the cognitive effects of S-ORC after MCAO/R in rats. In conclusion, α7nAChR and PI3K are key molecules that mediated the signaling pathway leading to S-ORC-induced cognitive restoration after MCAO/R.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Caveolin-1 promotes radioresistance in rhabdomyosarcoma through increased oxidative stress protection and DNA repair. (Pubmed Central) -  Sep 16, 2021   
    These findings were confirmed using radioresistant RD and RH30 lines generated by hypofractionated radiotherapy protocol, which showed marked increase of Cav-1, catalase and Akt, and sensitivity to PP2 and LY294002 treatment. In conclusion, these data suggest that concerted activity of Cav-1 and catalase, in cooperation with activation of Src-kinase and Akt pathways, may represent a network of vital mechanisms that allow irradiated RMS cells to evade cell death induced by oxidative stress and DNA damage.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  METTL14-regulated PI3K/Akt signaling pathway via PTEN affects HDAC5-mediated epithelial-mesenchymal transition of renal tubular cells in diabetic kidney disease. (Pubmed Central) -  Sep 15, 2021   
    Furthermore, HDAC5 expression was regulated by PI3K/Akt signaling pathway and inhibition of PI3K/Akt pathway by LY294002 treatment or Akt phosphorylation mutation reduced HDAC5 and TGF-β1 expression in vitro high glucose-cultured HK2 cells...Finally, in vivo HDACs inhibitor TSA treatment alleviated extracellular matrix accumulation in kidneys of diabetic mice, accompanied with HDAC5, TGF-β1, and α-SMA expression downregulation. These above data suggest that METTL14-regulated PI3K/Akt signaling pathway via PTEN affected HDAC5-mediated EMT of renal tubular cells in diabetic kidney disease.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, PD98059 / Wayne State University
    Journal:  HGF-mediated Up-regulation of PHLDA2 Is Associated With Apoptosis in Gastric Cancer. (Pubmed Central) -  Sep 15, 2021   
    OP 3-4 could promote bone regeneration of mandibular defect and improve osteogenic differentiation through protein kinase B/glycogen synthase kinase 3β/β-catenin pathway. PHLDA2 plays a role in gastric cancer tumorigenesis by inhibiting apoptosis through the PI3K/AKT pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Extracellular HSP90α Interacts With ER Stress to Promote Fibroblasts Activation Through PI3K/AKT Pathway in Pulmonary Fibrosis. (Pubmed Central) -  Sep 10, 2021   
    In addition, eHSP90α induced ER stress in fibroblasts via the phosphoinositide-4,5-bisphosphate 3-kinase (PI3K)-protein kinase B (AKT) signaling pathway, which could be blocked by the PI3K/AKT inhibitor LY294002, and blockade of eHSP90α by 1G6-D7 markedly inhibited ER stress in the model, indicating preventive and therapeutic applications...In conclusion, this study shows that the interaction between eHSP90α and ER stress plays a crucial role in pulmonary fibrosis, indicating a positive feedback in lung fibroblasts. Targeting eHSP90α and alleviating fibroblast ER stress may be promising therapeutic approaches for pulmonary fibrosis.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, Epigenetic controller:  Low-intensity pulsed ultrasound promotes angiogenesis via the AKT pathway and DNA methylation in human umbilical vein endothelial cells. (Pubmed Central) -  Sep 10, 2021   
    We observed that the expression of p-AKT was upregulated which means that the AKT signaling pathway could be activated by LIPUS, while inhibitor LY294002 of the AKT signaling pathway effectively blocked LIPUS-induced angiogenesis...Ourstudy demonstrated that LIPUS couldpromote the proliferation and angiogenic differentiation of ECs via the AKT signaling pathway. LIPUS could also alter DNA methylation of ECs via the activation of AKT signal.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Proteomic Analysis of Hypoxia-Induced Senescence of Human Bone Marrow Mesenchymal Stem Cells. (Pubmed Central) -  Sep 7, 2021   
    Hypoxia of hBMSCs inhibited CCND1 expression but promoted ROS production and cell apoptosis through activating the PI3K-dependent signaling pathway. These findings provided a detailed characterization of the proteomic profiles related to hypoxia-induced senescence of hBMSCs and facilitated our understanding of the molecular mechanisms leading to stem cell senescence.
  • ||||||||||  quercetin (LY294002) / Eli Lilly, Sutent (sunitinib) / Pfizer
    Journal:  Sensitizing endometrial cancer to ionizing radiation by multi-tyrosine kinase inhibition. (Pubmed Central) -  Sep 4, 2021   
    In conclusion, it is hoped that this combination will lead to a more specific targeted combination therapy that results in the abolition of AML. Our results provide the rationale of using sunitinib as neoadjuvant treatment prior radiotherapy which could be a starting point for the implementation of sunitinib and radiotherapy in the clinic for the treatment of recalcitrant endometrial cancers.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Autophagy drives fibroblast senescence through MTORC2 regulation. (Pubmed Central) -  Sep 4, 2021   
    Inhibition of senescence by shRNA to TP53/p53 and shRNA CDKN2A/p16 increased myofibroblast differentiation, suggesting a negative feedback loop of senescence on autophagy-induced myofibroblast differentiation. Collectively, our results identify ROS as central inducers of MTORC2 activation during chronic autophagy, which in turn fuels senescence activation and myofibroblast differentiation in distinct cellular subpopulations.Abbreviations: 3-MA: 3-methyladenine; ACTA2: actin, alpha 2, smooth muscle, aorta; AKT1: AKT serine/threonine kinase 1; p-AKT1: AKT1 Ser473 phosphorylation; t-AKT1: total AKT serine/threonine kinase 1; ATG4A: autophagy related 4A cysteine peptidase; ATG7: autophagy gene 7; C12FDG: 5-dodecanoylaminofluorescein Di-β-D-Galactopyranoside; CDKN1A: cyclin dependent kinase inhibitor 1A; CDKN2A: cyclin dependent kinase inhibitor 2A; Ctl: control; DAPI: 4',6-diamidino-2-phenylindole, dilactate; ECM: extracellular matrix; GSH: L-glutathione reduced; HO: hydrogen peroxide; HLF: adult human lung fibroblasts; Ho: Hoechst 33342 (2'-[4-ethoxyphenyl]-5-[4-methyl-1-piperazinyl]-2.5'-bi-1H-benzimidazole); HSC: hepatic stellate cells; LY: LY294002; MAP1LC3B/LC3B: microtubule-associated protein 1 light chain 3 beta; MTORC1/2: mechanistic target of rapamycin kinase complex 1/2; N: normal growth medium; NAC: N-acetyl-L-cysteine; PBS: phosphate-buffered saline; PDGFA: platelet derived growth factor subunit A; PRKCA/PKCα: protein kinase C alpha; PtdIns3K: class III phosphatidylinositol 3-kinase; PTEN: phosphatase and tensin homolog; R: rapamycin; RICTOR: RPTOR independent companion of MTOR complex 2; ROS: reactive oxygen species; RPTOR: regulatory associated protein of MTOR complex 1; SA-GLB1/β-gal: senescence-associated galactosidase beta 1; SGK1: serum/glucocorticoid regulated kinase 1; shRNA: short hairpin RNA; siCtl: control siRNA; siRNA: small interfering RNA; SQSTM1: sequestosome 1; SS: serum-free (serum starvation) medium; TP53: tumor protein p53; TUBA: tubulin alpha; V: vehicle.