product name
β-分泌酶抑制剂 IV, β-Secretase Inhibitor IV, CAS 797035-11-1, is a cell-permeable inhibitor that binds to BACE-1 active site and blocks its proteolytic activity (IC₅₀ = 15 nM for human BACE-1).
质量水平
检测方案
≥98% (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: 100 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C31H38N4O5S/c1-21(23-12-8-5-9-13-23)33-30(37)24-17-25(19-27(18-24)35(2)41(3,39)40)31(38)34-28(16-22-10-6-4-7-11-22)29(36)20-32-26-14-15-26/h4-13,17-19,21,26,28-29,32,36H,14-16,20H2,1-3H3,(H,33,37)(H,34,38)/t21-,28+,29-/m1/s1
InChI key
VPNIQGRFZCTBEZ-SPTGULJVSA-N
一般描述
一种细胞可渗透的有效抑制剂，与BACE-1活性位点结合并阻断其蛋白水解活性（BACE-1，人的IC50 = 15 nM，在HEK293-APPNFEV细胞中sAPP_NF的IC50=29 nM）。显示出比其他天冬氨酰蛋白酶更高的选择性（BACE-2、组织蛋白酶D和肾素的IC50分别为230 nM、7.6 µM和>50 µ M）。
一种细胞渗透性间苯二甲酰胺化合物，含有羟乙基胺基序，与BACE-1活性位点结合并能有效阻断其蛋白水解活性（BACE-1，人的IC50 = 15 nM，在HEK293-APPAPPNFEV细胞中sAPP_NF的IC50=29 nM）。显示出比其他天冬氨酰蛋白酶更高的选择性（BACE-2、组织蛋白酶D和肾素的IC50分别为0.23 µM、7.6 µM和>50 µM）。也可提供10 mM的DMSO溶液（目录号565794）。
请注意，由于水含量的变化，该化合物的分子量因批次而异。
请注意，由于水含量的变化，该化合物的分子量因批次而异。
生化/生理作用
主靶
BACE-1人
BACE-1人
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：BACE-1，人为15 nM，在HEK293-APPNFEV细胞中的sAPP_NF为29 nM
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3个月。
其他说明
Halima, S.B., et al. 2016.Cell Reports.14, In press.
Stachel, S.J., et al. 2004.J. Med. Chem.47, 6447.
Stachel, S.J., et al. 2004.J. Med. Chem.47, 6447.
在DMSO（10 mg/ml）中溶解，等分&贮藏在-20℃下；可稳定3个月。
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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