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推荐产品
product name
γ-分泌酶抑制剂XXI，化合物E, 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
检测方案
≥95% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C27H24F2N4O3/c1-16(30-23(34)14-17-12-19(28)15-20(29)13-17)26(35)32-25-27(36)33(2)22-11-7-6-10-21(22)24(31-25)18-8-4-3-5-9-18/h3-13,15-16,25H,14H2,1-2H3,(H,30,34)(H,32,35)/t16-,25?/m0/s1
InChI key
JNGZXGGOCLZBFB-YPHZTSLFSA-N
一般描述
γ-分泌酶和Notch加工的一种细胞可渗透的、有效的、选择性的、拟肽的、非过渡态类似物抑制剂（在过表达野生型βAPP的CHO细胞中，Aβ40的IC50为300 pM；在用βAPP695和mNotchΔE(M1727V)稳定转染的HEK293细胞中，Aβ40、Aβ42、NICD的IC50分别为240 pM、370 pM、320 pM；在SPA4CT稳定转染的SH-SY5Y细胞中，Aβ40和Aβ42的IC50为100 pM）在几个APP转基因小鼠模型中降低Aβ水平。据报道，与早老素结合并抑制跨膜蛋白底物的蛋白水解裂解，包括APLP1和APLP2、CD44、ErbB4、E-钙粘蛋白、低密度脂蛋白受体相关蛋白、Notch配体和p75NTR。在更高浓度（200-400 µM）下，对早老酶活性的影响很弱。
生化/生理作用
主要靶标
过表达野生型bAPP的CHO细胞中的γ-分泌酶和Notch加工Ab40
过表达野生型bAPP的CHO细胞中的γ-分泌酶和Notch加工Ab40
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：在过表达野生型βAPP的CHO细胞中，对于Aβ40，为300 pM；在用βAPP695和mNotchΔE(M1727V)稳定转染的HEK293细胞中，对于Aβ40、Aβ42、NICD，分别为240 pM、370 pM、320 pM；对于Aβ40为100 pM
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。
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.
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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