产品说明书
L-685458
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同义名 : | γ-Secretase Inhibitor X;L-685,458;L685,458, L-685,458 |
| CAS号 : | 292632-98-5 | |
| 货号 : | A142296 | |
| 分子式 : | C39H52N4O6 | |
| 纯度 : | 99%+ | |
| 分子量 : | 672.853 | |
| MDL号 : | MFCD03093402 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 85 mg/mL(126.33 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | L-685458 serves as a potent γ-secretase inhibitor (GSI), classified as a transition state analog (TSA), and effectively inhibits amyloid β-protein precursor γ-secretase activity with an IC50 of 17 nM, displaying more than 50-100-fold selectivity against other tested aspartyl proteases. This compound impedes γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50 values of 301.3 nM and 351.3 nM, respectively, and is investigated for its potential in Alzheimer’s disease (AD) and cancer research[1].[2]. | ||
| 作用机制 | L-685458 is an aspartyl protease transition state mimic which exhibits stereoselectivity to AβPP γ-secretase activity with much less potency to aspartyl, serine, and cysteine protease activity, thereby abolishing the formation of all Aβ peptide species.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.49mL 0.30mL 0.15mL |
7.43mL 1.49mL 0.74mL |
14.86mL 2.97mL 1.49mL |
| 参考文献 |
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[1]Shearman, M.S., Beher, D., Clarke, E.E., Lewis, H.D., Harrison, T., Hunt, P., |