merck millipore,默克密理博,565790,γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4

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merck millipore,默克密理博,565790,γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem
产品名称：γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem
产品型号：565790
The γ-Secretase Inhibitor XXI, Compound E, also referenced under CAS 209986-17-4, controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience appl More>>

merck millipore,默克密理博,565790,γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem

产品介绍

merck millipore,默克密理博,565790,γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem

重要规格表

经验配方	CAS号
C₂₇H₂₄F₂N₄O₃	209986-17-4

描述
概述	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 p75^NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM).
产品目录编号	565790
品牌系列	Calbiochem®
同义词	(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

参考
参考	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. Oncogene 22, 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. Science 294, 2179. Beher, D., et al. 2001. J. Biol. Chem. 276, 45394. Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312. Seiffert, D., et al. 2000. J. Biol. Chem. 275, 34086.

参考

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. Oncogene 22, 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. Science 294, 2179.
Beher, D., et al. 2001. J. Biol. Chem. 276, 45394.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312.
Seiffert, D., et al. 2000. J. Biol. Chem. 275, 34086.

产品信息
CAS号	209986-17-4
具有ATP竞争性	N
形式	White solid
Hill配方	C₂₇H₂₄F₂N₄O₃
化学配方	C₂₇H₂₄F₂N₄O₃
Molar Mass	490.5
可逆	N
结构配方图像

生物信息
主靶	γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
主靶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
纯度	≥95% by HPLC

理化信息
细胞可渗透	Y
溶解度	DMSO

储存和货运信息
货运代码	Ambient Temperature Only
毒性	Standard Handling
储存	+2°C to +8°C
避光	Protect from light
无需冷冻	No
特殊指南	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.