货号 | 13127-500ug |
描述 | Neutral sphingomyelinases mediate the release of ceramide from sphingomyelin in cellular membranes and can be activated by certain stresses. Ceramide can act as a signaling molecule in its own right, or it can be further processed to generate sphingosine (and sphingosine-1-phosphate). GW 4869 is a cell-permeable, non-competitive inhibitor of neutral sphingomyelinases (IC50 = 1 μM), but does not affect acid sphingomyelinase activity.1 It inhibits TNF-α-mediated sphingomyelin hydrolysis (100% inhibition at 20 μM) 1 and TNF-α-induced cell death in MCF-7 cells without interfering with activation of NF-κB or glutathione depletion in response to TNF.1,2 GW 4869 also reduces the inhibitory effect of oxidized phospholipid products on lipopolysaccharides-mediated induction of interleukin-8 in human aortic endothelial cells 3 and prevents hypoxia-induced pulmonary vasoconstriction in rats in vivo.4 |
供应商 | Cayman |
应用文献 | |
1.Luberto, C.,Hassler, D.F.,Signorelli, P., et al. Inhibition of tumor necrosis factor-induced cell death in MCF7 by a novel inhibitor of neutral sphingomyelinase. The Journal of Biological Chemisty 277(43), 41128-41139 (2002). 2.Marchesini, N.,Luberto, C. and Hannun, Y.A. Biochemical properties of mammalian neutral sphingomyelinase2 and its role in sphingolipid metabolism. The Journal of Biological Chemisty 278(16), 13775-13783 (2003). 3.Walton, K.A.,Gugiu, B.G.,Thomas, M., et al. A role for neutral sphingomyelinase activation in the inhibition of LPS action by phospholipid oxidation products. Journal of Lipid Research 47, 1967-1974 (2006). 4.Cogolludo, A.,Moreno, L.,Frazziano, G., et al. Activation of neutral spingomyelinase is involved in acute hypoxic pulmonary vasoconstriction. Cardiovascular Research 82, 296-302 (2009). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥90% |
计算分子量 | 577.5 |
分子式 | C30H28N6O2 • 2HCl [XH2O] |
CAS号 | 6823-69-4 |
稳定性 | ≥ 2 years |
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