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γ-Secretase Inhibitor XXI, Compound E-CAS 209986-17-4-Calbiochem
| 产品编号： | 4073889 |
| 规格： | This g-secretase inhibitor, CAS 209986-17-4, is a cell-permeable, potent, selective, non-transition-state analog inhibitor of γ-secretase and Notch processing. Lowers Aβ levels in APP transgenic mice |
| CAS NO： | 209986-17-4 |
| 包装规格： | 500 μG，1 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品价格查看更多规格...
| 产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
| 4073889 | 500 μG | 4480 | |||
| 4073889 | 1 MG | 5810 |
产品别名
209986-17-4
γ-Secretase Inhibitor XXI, Compound E-CAS 209986-17-4-Calbiochem
(S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, Compound E
基本信息
| Empirical Formula【经验(实验)分子式】 | C27H24F2N4O3 |
| Molecular weight | 490.50 |
| General description【一般描述】 | A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC50 = 300 pM for Aβ40 in CHO cells overexpressing wild type βAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40 and Aβ42 in SH-SY5Y cells stably transfected with SPA4CT). Lowers Aβ levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM). |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Target IC50: 300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40 Primary Target γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP Product does not compete with ATP. Reversible: no |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Milano, J., et al. 2004. Toxicol. Sci.82, 341. Jung, K.M., et al. 2003. J. Biol. Chem.278, 42161. Murakami, D., et al. 2003. Oncogene22, 1511. Campbell, W.A., et al. 2003. J. Neurochem.85, 1563. Berechid, B.E., et al., 2002. J. Biol. Chem.277, 8154. Lee, H.J., et al. 2002. J. Biol. Chem.277, 6318. May, P., et al. 2002. J. Biol. Chem.277, 18736. Scheinfeld, M.H., et al. 2002. J. Biol. Chem.277, 44195. Ni, C. Y., et al. 2001. Science294, 2179. Beher, D., et al. 2001. J. Biol. Chem.276, 45394. Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312. Seiffert, D., et al. 2000. J. Biol. Chem.275, 34086. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥95% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | white |
| solubility【溶解性】 | DMSO: 10 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 500 μg in Plastic ampoule 1 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
