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product name
γ-分泌酶抑制剂IIX, Gamma-Secretase Inhibitor IX - CAS 208255-80-5, is a cell-permeable inhibitor of γ-secretase (Aβtotal IC₅₀ = 115 nM, Aβ42 IC₅₀ = 200 nM).
质量水平
检测方案
≥98% (HPLC)
形式
lyophilized
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
溶解性
DMSO: 20 mg/mL
运输
ambient
储存温度
−20°C
InChI
1S/C23H26F2N2O4/c1-14(26-19(28)12-15-10-17(24)13-18(25)11-15)21(29)27-20(16-8-6-5-7-9-16)22(30)31-23(2,3)4/h5-11,13-14,20H,12H2,1-4H3,(H,26,28)(H,27,29)/t14-,20-/m0/s1
InChI key
DWJXYEABWRJFSP-XOBRGWDASA-N
一般描述
一种可渗透细胞的二肽，通过阻断γ-分泌酶来抑制Aβ的产生（Aβ总IC50 = 115 nM，Aβ42 IC50 = 200 nM）。在小鼠N2a细胞和hAPP/hBACE-1转染的人HEK 293细胞中阻止Aβ34生成。据报道，在HEK 293细胞和神经元培养中均具有功能活性，且不影响淀粉-β样前体蛋白（APP）的分泌。在APP转基因小鼠中也显示出显著降低Aβ水平。据报道，可减少3xTgAD 转基因小鼠的细胞外Aβ斑块和细胞内Aβ积累。也可提供25 mM(5 mg/462 µl) γ-分泌酶抑制剂IX（目录号565784）在DMSO中的溶液。
一种细胞渗透性二肽，抑制γ-分泌酶活性并抑制Aβ的产生（Aβ总IC50 = 115 nM；Aβ42 IC50 = 200 nM)。据报道，在过度表达人APP751的HEK293细胞和神经元培养物中都具有功能活性，但是，它不影响淀粉样蛋白b前体蛋白（APP）的分泌。在急性降低APPV717F转基因小鼠的抗体方面有效。在稳定转染瑞典突变体βAPP695的HEK293细胞中，也能有效抑制~6 kDa C-末端裂解产物（CTFg）的产生。据报道，可减少3xTgAD 转基因小鼠的细胞外Aβ斑块和细胞内Aβ积累。
生化/生理作用
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：115nm抑制Aβ总计产生；200 nM抑制Aβ42的产生
包装
用惰性气体包装
警告
毒性：标准处理（A）
其他说明
Morohashi, Y., et al. 2006.J. Bio.Chem.Vol.281, 14670.
Nishitomo, K. et al. 2006 J. Neurochem.99, 1555.
Oddo, S., et al. 2004.Neuron43, 321.
Dovey, H.F., et al. 2001.J. Neurochem.76, 173.
Sastre, M., et al. 2001.EMBO Rep.2, 835.
Vandermeeren, M., et al. 2001.Neurosci. Lett.315, 145.
Nishitomo, K. et al. 2006 J. Neurochem.99, 1555.
Oddo, S., et al. 2004.Neuron43, 321.
Dovey, H.F., et al. 2001.J. Neurochem.76, 173.
Sastre, M., et al. 2001.EMBO Rep.2, 835.
Vandermeeren, M., et al. 2001.Neurosci. Lett.315, 145.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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