LY294002 / Eli Lilly 
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  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Expression of ARID1A in polycystic ovary syndrome and its effect on the proliferation and apoptosis of ovarian granulosa cells. (Pubmed Central) -  Nov 6, 2021   
    These results suggest that lipid emulsion inhibits late apoptosis induced by amlodipine at toxic dose via the activation of phosphoinositide-3 kinase and ATP-sensitive potassium channels in the extrinsic apoptotic pathway. ARID1A was down-regulated in GCs cells form PCOS women and from PCOS animal models, while ARID1A overexpression can suppress the PI3K/Akt pathway to inhibit proliferation and promote apoptosis in ovarian granulosa cells.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO biomarker:  Effect of pyrroloquinoline quinone on lipopolysaccharide-induced autophagy in HAPI microglia cells. (Pubmed Central) -  Nov 5, 2021   
    The phosphatidylinositol 3-kinase (PI3K)/Akt inhibitor LY294002 was used to block the Akt pathway...In LPS-induced HAPI microglia, PQQ reduces the apoptosis level and increases that of autophagy. In addition, PQQ changes the distribution of LAMP2 in the cytoplasm and nucleus, which is regulated through the PI3K/Akt signaling pathway.
  • ||||||||||  LY294002 / Eli Lilly
    Anti-Apoptotic Effect of Angelica Polysaccharide (APS) on Cryopreservation of Platelets (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_4922;    
    The effects of APS on cells treated with Ly294002, PI3K inhibitor and the effect of APS on the p-AKT were also studied... APS, like TPO, has an anti-apoptotic effect on the cryopreserved platelets and megakaryocytes through activating PI3K/AKT, decreasing the expression of Caspase-3 and inhibiting the reduction of MMP.
  • ||||||||||  Venclexta (venetoclax) / Roche, AbbVie, quercetin (LY294002) / Eli Lilly
    Journal, IO biomarker:  Synergistic effects of LY294002 and ABT199 on the cell cycle in K562, HL60 and KG1a cells. (Pubmed Central) -  Nov 5, 2021   
    At the molecular level, LY294002 and ABT199 combination treatment significantly downregulated Skp2, Bcl2, procaspase‑3 and procaspase‑9 expression levels, but markedly upregulated p27, Bax, cleaved caspase‑3 and caspase‑9 expression levels in K562, HL‑60 and KG1a cells. The results of the present study demonstrated that LY294002 and ABT199 combination treatment may serve as a novel therapeutic strategy for AML.
  • ||||||||||  MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly
    Journal:  Hederagenin Protects PC12 Cells Against Corticosterone-Induced Injury by the Activation of the PI3K/AKT Pathway. (Pubmed Central) -  Nov 1, 2021   
    In line with this, western blot analysis results showed that Hederagenin stimulated the phosphorylation of AKT and its downstream target Forkhead box class O 3a (FoxO3a) and Glycogen synthase kinase-3-beta (GSK3β) in a concentration dependent manner. Taken together, these results indicate that the neuroprotective effect of Hederagenin is likely to occur via stimulation of the PI3K/AKT pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Spermidine-induced improvement of memory consolidation involves PI3K/Akt signaling pathway. (Pubmed Central) -  Oct 31, 2021   
    We found that SPD improved fear memory consolidation and that both ANA-12 and LY294002 prevented the facilitatory effect of SPD on memory. These results suggest that SPD-induced improvement of memory consolidation involves the activation of the TrkB receptor and PI3K/Akt pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Apelin ameliorated acute heart failure via inhibiting endoplasmic reticulum stress in rabbits. (Pubmed Central) -  Oct 30, 2021   
    The Akt signaling inhibitors wortmannin and LY294002 could block the cardioprotective effect of apelin, which could be relieved by ERS inhibitor 4-phenyl butyric acid (4-PBA)...Apelin treatment dramatically ameliorated cardiac impairment caused by AHF, which might be mediated by APJ/Akt/ERS signaling pathway. These results will shed new light on AHF therapy.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  PI3K/AKT phosphorylation activates ERRα by upregulating PGC‑1α and PGC‑1β in gallbladder cancer. (Pubmed Central) -  Oct 29, 2021   
    LY294002 and insulin‑like growth factor I (IGF‑I) were used to inhibit and promote PI3K/AKT phosphorylation, respectively...Moreover, knockdown of PGC‑1α and PGC‑1β antagonized ERRα activation, which was enhanced by PI3K/AKT phosphorylation. Taken together, the present study demonstrated that PI3K/AKT phosphorylation triggered ERRα by upregulating the expression levels of PGC‑1α and PGC‑1β in NOZ cells.
  • ||||||||||  Mekinist (trametinib) / Novartis, LY294002 / Eli Lilly
    Heterogeneity of preneoplastic breast tissues drives efficacy of therapeutic agents (Hall 1) -  Oct 26, 2021 - Abstract #SABCS2021SABCS_734;    
    Effectiveness of targeted drug therapies in this model of breast tumorigenesis correlated with deregulation of the associated pathway. This implies that accounting for heterogeneity of the preneoplastic breast and stage of tumorigenic progression will be important when considering targeted strategies for prevention.
  • ||||||||||  Xalkori (crizotinib) / Pfizer, quercetin (LY294002) / Eli Lilly
    Journal:  HGF protected against diabetic nephropathy via autophagy-lysosome pathway in podocyte by modulating PI3K/Akt-GSK3β-TFEB axis. (Pubmed Central) -  Oct 22, 2021   
    Accordingly, adenovirus vector encoding constitutively active GSK3β (Ad-GSK3β-S9A) offset whereas small interfering RNA against GSK3β (GSK3β siRNA) recapitulated salutary effects of HGF on lysosome number and autophagy in podocytes. These results suggested that HGF protected against diabetic nephropathy through restoring podocyte autophagy, which at least partially involved PI3K/Akt-GSK3β-TFEB axis-mediated lysosomal function improvement.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Poly(I:C) preconditioning protects the heart against myocardial ischemia/reperfusion injury through TLR3/PI3K/Akt-dependent pathway. (Pubmed Central) -  Oct 16, 2021   
    Moreover, inhibition of p85 PI3K by the administration of LY294002 in vivo and knockdown of Akt by siRNA in vitro significantly abolish poly(I:C) preconditioning-induced cardioprotective effect. In conclusion, our results reveal that poly(I:C) preconditioning exhibits essential protection in myocardial I/R injury via its modulation of TLR3, and the downstream PI3K/Akt signaling, which may provide a potential pharmacologic target for perioperative cardioprotection.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  LY‑294002 enhances the chemosensitivity of liver cancer to oxaliplatin by blocking the PI3K/AKT/HIF‑1α pathway. (Pubmed Central) -  Oct 14, 2021   
    The present study investigated the effects of the PI3K inhibitor LY‑294002 and AKT inhibitor MK2206 on the chemosensitivity of oxaliplatin‑resistant liver cancer cells and the molecular mechanism involved...It was concluded that LY‑294002 enhanced the chemosensitivity of liver cancer cells to oxaliplatin by inhibiting the PI3K/AKT signaling pathway, which may be related to the inhibition of HIF‑1α expression. These findings may have clinical significance for the treatment of oxaliplatin‑resistant liver cancer.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  The Effect of si-PKM2 on Proliferation and Apoptosis of Acute Leukemic Cells and Its Molecular Mechanism (Pubmed Central) -  Oct 12, 2021   
    FDXR could serve as a potential marker of advanced sebaceous differentiation, and its overexpression may be involved in the development of acne lesions. PKM2 knockdown can inhibit the proliferation and induce apoptosis of HL-60 cells, and its molecular mechanism may be related to the PKM2-mediated PI3K/Akt/mTOR-glycolysis, which suggesting that PKM2 may serve as a molecular target for the prevention and treatment of leukemia.
  • ||||||||||  metamizole / Generic mfg.
    Journal:  9The PI3Kγ/AKT signaling pathway mediates peripheral antinociceptive action of dipyrone. (Pubmed Central) -  Oct 10, 2021   
    Corroborating these data, we found that DIP induced AKT phosphorylation in cultured dorsal root ganglion neurons, which was prevented in the presence of PI3Kγ selective inhibitor. Taken together, these findings provide evidence that peripheral analgesic effect of DIP is dependent on the activation of PI3Kγ/AKT signaling pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal:  Role of phosphatidylinositol 3-kinase signaling pathway in radiation-induced liver injury. (Pubmed Central) -  Oct 9, 2021   
    However, the expression of TGF-β1, Akt, and α-SMA were significantly decreased in PI3K/Akt signal pathway inhibitor LY294002-treated group. Our results suggest that during radiation-induced liver injury, HSCs are activated by TGF-β1-mediated PI3K/Akt signal pathway.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO biomarker:  Loganin Attenuates Septic Acute Renal Injury with the Participation of AKT and Nrf2/HO-1 Signaling Pathways. (Pubmed Central) -  Oct 8, 2021   
    Finally, AKT blockage by 10 μM LY294002 or Nrf2 inhibition by10 μ M ML385 were utilized to prove the involvement of AKT and Nrf2/HO-1 pathway in AKI during sepsis...Besides, the protective effects of Loganin could be diminished by AKT or Nrf2 blockage, indicating the involvement of AKT and Nrf2/HO-1 pathway. The results suggested that the protective effects of Loganin on AKI during sepsis might be mediated by AKT and Nrf2/HO-1 pathway signaling activation in kidney proximal tubular cells.
  • ||||||||||  Kadcyla (ado-trastuzumab emtansine) / Roche
    Journal:  Targeting the autophagy promoted antitumor effect of T-DM1 on HER2-positive gastric cancer. (Pubmed Central) -  Oct 7, 2021   
    Furthermore, autophagic inhibition might increase the fusion of T-DM1 with lysosomes, which might accelerate the release of the cytotoxic molecule emtansine from the T-DM1 conjugate. These findings highlight a promising therapeutic strategy that combines T-DM1 with an autophagy inhibitor to treat HER-positive GC more efficiently.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Journal, IO biomarker:  The protective effect of decoction of Rehmanniae via PI3K/Akt/mTOR pathway in MPP-induced Parkinson's disease model cells. (Pubmed Central) -  Oct 6, 2021   
    To further determine the protective effect of DOR on acute injury via PI3K/Akt/mTOR pathway, cells were treated with LY294002 (LY), a PI3K/Akt/mTOR pathway inhibitor, with MMP + or DOR or not...DOR had a protective effect against MPP induced injury of Parkinson's disease model cell through activating the PI3K/Akt/mTOR pathway. It suggests that DOR should be further explored in Parkinson's disease.
  • ||||||||||  cisplatin / Generic mfg., sirolimus / Generic mfg., paclitaxel / Generic mfg.
    Journal, Cancer stem cells:  Survival of salivary gland cancer stem cells requires mTOR signaling. (Pubmed Central) -  Oct 6, 2021   
    Using a panel of inhibitors of the mTOR pathway, i.e., rapamycin and temsirolimus (mTOR inhibitors), buparlisib and LY294002 (AKT inhibitors), and PF4708671 (S6K1 inhibitor), we observed consistently dose-dependent decrease in the fraction of CSC, as well as inhibition of secondary sphere formation and self-renewal in three human MEC cell lines (UM-HMC-1,-3A,-3B)...In contrast, conventional chemotherapeutic drugs (cisplatin, paclitaxel) induced preferential apoptosis of bulk tumor cells and accumulation of CSC...Transplantation of MEC cells genetically silenced for mTOR into immunodeficient mice corroborated the results obtained with temsirolimus. Collectively, these data demonstrated that mTOR signaling is required for CSC survival, and unveiled the therapeutic potential of targeting the mTOR pathway for elimination of highly tumorigenic cancer stem-like cells in salivary gland mucoepidermoid carcinoma.
  • ||||||||||  dexamethasone / Generic mfg.
    Preclinical, Journal:  Elevated levels of expression of cytochrome P450 3A4 in a human liver epithelial cell line in differentiation-inducing conditions. (Pubmed Central) -  Oct 6, 2021   
    The mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) inhibitor U0126 or the phosphatidylinositol-3-kinase (PI3K) inhibitor LY294002 reduced CYP3A4 mRNA levels of THLE-5b cells...In conclusion, THLE-5b cells, which are unmethylated at the CpG site of the CYP3A4 promoter region, express CYP3A4 mRNA through the MEK/ERK1/2 and PI3K/Akt signaling pathways and acquire hepatocytic functions in differentiation-inducing conditions. Thus, THLE-5b cells could be a useful cell system for the study of drug metabolism.
  • ||||||||||  quercetin (LY294002) / Eli Lilly
    Preclinical, Journal:  Regulation mechanism of miR-494-3p on endometrial receptivity in mice via PI3K/AKT/mTOR pathway. (Pubmed Central) -  Oct 5, 2021   
    Subsequently, human endometrial epithelial cells (hEECs) were transfected with miR-494-3p inhibitor and PI3K inhibitor (LY294002)...Overall, these results suggested that miR-494-3p is the key regulator of endometrial receptivity in mice, regulating this complex process through the PI3K/AKT/mTOR pathway. Understanding the role of miR-494-3p in endometrial receptivity is of great significance for exploring new targets for the diagnosis and treatment of early pregnancy failure, and improving the success rates of artificial reproduction.
  • ||||||||||  MK-2206 / Merck (MSD), quercetin (LY294002) / Eli Lilly
    Journal:  Intervention of Gastrodin in Type 2 Diabetes Mellitus and Its Mechanism. (Pubmed Central) -  Oct 5, 2021   
    Our results indicate that gastrodin promotes the phosphorylation of GATA1 via the PI3K/AKT pathway, enhances the transcriptional activity of GATA1, and then increases the expression level of USP4, thereby reducing the ubiquitination and degradation of insulin receptors and ultimately improving insulin resistance. Our study provides scientific evidence for the beneficial actions and underlying mechanism of gastrodin in the treatment of T2DM.