LY294002 - CAS 154447-36-6
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Not Intended for Therapeutic Use. For research use only.
LY294002 is a potent inhibitor of phosphoinositide PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively.
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1.Hydrogen sulfide protects H9c2 cardiac cells against doxorubicin-induced cytotoxicity through the PI3K/Akt/FoxO3a pathway.
Liu MH1, Zhang Y2, He J1, Tan TP1, Wu SJ1, Guo DM3, He H4, Peng J4, Tang ZH4, Jiang ZS4. Int J Mol Med. 2016 Apr 14. doi: 10.3892/ijmm.2016.2563. [Epub ahead of print]
Doxorubicin (DOX) is an efficient drug used in cancer therapy that also produces reactive oxygen species (ROS) that induces severe cytotoxicity, which limits its clinical application. Hydrogen sulfide (H2S), a novel gasotransmitter, has been shown to exert cardioprotective effects. The present study aimed to determine whether exogenous H2S protects H9c2 cardiac cells against DOX-induced cytotoxicity and whether these protective effects are mediated through the PI3K/Akt/FoxO3a pathway. The H9c2 cardiac cells were exposed to 5 µM DOX for 24 h to establish a model of DOX-induced cardiotoxicity. The results showed that the treatment of H9c2 cardiac cells with sodium hydrosulfide (NaHS) for 30 min prior to DOX exposure markedly attenuated the phosphorylation of Akt and FoxO3a. Notably, pre-treatment of the H9c2 cells with NaHS significantly attenuated the nuclear localization of FoxO3a as well as the apoptosis of H9c2 cells induced by DOX. The treatment of H9c2 cells with N-acetyl-L-cysteine (NAC), a scavenger of ROS, prior to DOX exposure, also markedly increased the phosphorylation of Akt and FoxO3a which was inhibited by DOX alone.
2.Neuroprotective and antioxidant activities of bamboo salt soy sauce against H2O2-induced oxidative stress in rat cortical neurons.
Jeong JH1, Noh MY2, Choi JH3, Lee H4, Kim SH2. Exp Ther Med. 2016 Apr;11(4):1201-1210. Epub 2016 Feb 9.
Bamboo salt (BS) and soy sauce (SS) are traditional foods in Asia, which contain antioxidants that have cytoprotective effects on the body. The majority of SS products contain high levels of common salt, consumption of which has been associated with numerous detrimental effects on the body. However, BS may be considered a healthier substitute to common salt. The present study hypothesized that SS made from BS, known as bamboo salt soy sauce (BSSS), may possess enhanced cytoprotective properties; this was evaluated using a hydrogen peroxide (H2O2)-induced neuronal cell death rat model. Rat neuronal cells were pretreated with various concentrations (0.001, 0.01, 0.1, 1 and 10%) of BSSS, traditional soy sauce (TRSS) and brewed soy sauce (BRSS), and were subsequently exposed to H2O2 (100 µM). The viability of neuronal cells, and the occurrence of DNA fragmentation, was subsequently examined. Pretreatment of neuronal cells with TRSS and BRSS reduced cell viability in a concentration-dependent manner, whereas neuronal cells pretreated with BSSS exhibited increased cell viability, as compared with non-treated neuronal cells.
3.NGF increases VEGF expression and promotes cell proliferation via ERK1/2 and AKT signaling in Müller cells.
Wang J1, He C1, Zhou T1, Huang Z1, Zhou L1, Liu X1. Mol Vis. 2016 Mar 25;22:254-63. eCollection 2016.
PURPOSE: Nerve growth factor (NGF) is a classic neuroprotective factor that contributes to angiogenesis under pathological conditions, which might be mediated by the upregulation of vascular endothelial growth factor (VEGF). Retinal Müller cells are a critical source of growth factors, including NGF and VEGF, and express the receptor for NGF, indicating the functional significance of NGF signaling in Müller cells. The aim of this study is to explore the effect of NGF on the production of other growth factors and cellular proliferation in Müller cells and to further detect the potential mechanism of these effects.
4.Ursolic acid induced anti-proliferation effects in rat primary vascular smooth muscle cells is associated with inhibition of microRNA-21 and subsequent PTEN/PI3K.
Jiang Q1, Han Y1, Gao H1, Tian R1, Li P2, Wang C3. Eur J Pharmacol. 2016 Apr 13. pii: S0014-2999(16)30205-9. doi: 10.1016/j.ejphar.2016.04.001. [Epub ahead of print]
This study focused on the anti-proliferation effects of ursolic acid (UA) in rat primary vascular smooth muscle cells (VSMCs) and investigated underlying molecular mechanism of action. Rat primary VSMCs were pretreated with UA (10, 20 or 30μM) or amino guanidine (AG, 50μM) for 12h or with PI3K inhibitor LY294002 for 30min or with Akt inhibitor MK2206 for 24h, then 10% fetal bovine serum was used to induce proliferation. CCK-8 was used to assess cell proliferation. To explore the mechanism, cells were treated with UA (10, 20 or 30μM), LY294002 or MK2206, or transient transfected to inhibit miRNA-21 (miRNA-21) or to overepxress PTEN, then quantitative real-time PCR was used to assess the mRNA levels of miRNA-21 and phosphatase and tensin homolog (PTEN) for cells treated with UA or miRNA-21 inhibitor; western blotting was used to measure the protein levels of PTEN and PI3K. UA exerted significant anti-proliferation effects in rat primary VSMCs.
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