| 货号 | 13197-50mg |
| 描述 | γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.1 DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.1,2,3 Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.4,5 |
| 别名 | GSI-IX; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Dovey, H.F.,John, V.,Anderson, J.P., et al. Functional γ-secretase inhibitors reduce β-amyloid peptide levels in brain. Journal of Neurochemistry 76, 173-181 (2001). 2.Portelius, E.,Zhang, B.,Gustavsson, M.K., et al. Effects of γ-secretase inhibition on the amyloid β isoform pattern in a mouse model of Alzheimer’s disease. Neurodegener.Dis. 6, 258-262 (2009). 3.El Mouedden, M.,Vandermeeren, M.,Meert, T., et al. Reduction of Aβ levels in the Sprague Dawley rat after oral administration of the functional γ-secretase inhibitor, DAPT: A novel non-transgenic model for Aβ production inhibitors. Current Pharmaceutical Design 12, 671-676 (2006). 4.Kanungo, J.,Zheng, Y.L.,Amin, N.D., et al. The Notch signaling inhibitor DAPT down-regulates cdk5 activity and modulates the distribution of neuronal cytoskeletal proteins. Journal of Neurochemistry 106, 2236-2248 (2008). 5.De Smedt, M.,Hoebeke, I.,Reynvoet, K., et al. Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironment. Blood 106(10), 3498-3506 (2005). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 432.5 |
| 分子式 | C23H26F2N2O4 |
| CAS号 | 208255-80-5 |
| 稳定性 | ≥ 2 years |
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