| 货号 | 15579-1mg |
| 描述 | γ-Secretase is a multimeric aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules.1 Two well-known substrates are the carboxyl-terminal fragments (CTFs) of the receptor Notch, which has key roles in development, and that of amyloid precursor protein (APP), which is important in Alzheimer’s disease.1 Compound E is a potent, cell-permeable, and selective inhibitor of γ-secretase, blocking the cleavage of both APP and Notch CTFs with IC50 values of ~0.3 nM.2,3,4 Compound E induces neuronal differentiation, impairs ovarian folliculogenesis, and suppresses thymocyte development by preventing Notch activation by γ-secretase.5,6,7 |
| 别名 | γ-Secretase Inhibitor XXI; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jurisch-Yaksi, N.,Sannerud, R. and Annaert, W. A fast growing spectrum of biological functions of γ-secretase in development and disease. Biochim Biophys.Acta. 1828(12), 2815-2827 (2013). 2.Seiffert, D.,Bradley, J.D.,Rominger, C.M., et al. Presenilin-1 and -2 are molecular targets for γ-secretase inhibitors. The Journal of Biological Chemisty 275(44), 34086-34091 (2000). 3.Beher, D.,Wrigley, J.D.J.,Nadin, A., et al. Pharmacological knock-down of the presenilin 1 heterodimer by a novel g -secretase inhibitor. Implications for presenilin biology. The Journal of Biological Chemisty 276(48), 45394-45402 (2001). 4.Zhao, G.,Mao, G.,Tan, J., et al. Identification of a new presenilin-dependent ζ-cleavage site within the transmembrane domain of amyloid precursor protein. The Journal of Biological Chemisty 279(49), 50647-50650 (2004). 5.Ferrari-Toninelli, G.,Bonini, S.A.,Uberti, D., et al. Targeting Notch pathway induces growth inhibition and differentiation of neuroblastoma cells. Neuro.Oncol. 12(12), 1231-1243 (2010). 6.Jovanovic, V.P.,Sauer, C.M.,Shawber, C.J., et al. Intraovarian regulation of gonadotropin-dependent folliculogenesis depends on notch receptor signaling pathways not involving Delta-like ligand 4 (Dll4). Reproductive Biology and Endocrinology 11, 43 (2013). 7.Doerfler, P.,Shearman, M.S. and Perlmutter, R.M. Presenilin-dependent γ-secretase activity modulates thymocyte development. Proceedings of the National Academy of Sciences of the United States of America 98(16), 9312-9317 (2001). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 490.5 |
| 分子式 | C27H24F2N4O3 |
| CAS号 | 209986-17-4 |
| 稳定性 | ≥ 2 years |
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