565771
γ-Secretase Inhibitor X
≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem®
别名:
InSolution γ-Secretase Inhibitor X, L-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester
产品名称
γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
质量水平
方案
≥90% (HPLC)
表单
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated
protect from light
运输
ambient
储存温度
−20°C
相关类别
一般描述
A cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of γ-secretase (Aβ total IC50 = 17 nM; Aβ40 IC50 = 48 nM; and Aβ42 IC50 = 67 nM in SH-SY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Also reported to block the formation of εCTF, resulting in the accumulation of α- and βCTF. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D.
生化/生理作用
Cell permeable: yes
Primary Target
Aβtotal
Aβtotal
Product does not compete with ATP.
Reversible: no
Target IC50: Aβtotal 17 nM, Aβ40 48 nM, and Aβ42 67 nM in SHSY5Y cells overexpressing spβA4CTF
包装
Packaged under inert gas
外形
A 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.
制备说明
Following initial thaw, aliquot and freeze (-20°C).
其他说明
Weidemann, A., et al. 2002. Biochemistry41, 2825.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312.
Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA97, 6138.
Shearman, M.S., et al. 2000. Biochemistry39, 8698.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312.
Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA97, 6138.
Shearman, M.S., et al. 2000. Biochemistry39, 8698.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
10 - Combustible liquids
WGK
WGK 1
闪点(°F)
188.6 °F - closed cup - (Dimethylsulfoxide)
闪点(°C)
87 °C - closed cup - (Dimethylsulfoxide)
Sylvia M Lee et al.
Cancer, 121(3), 432-440 (2014-09-25)
Aberrant Notch activation confers a proliferative advantage to many human tumors, including melanoma. This phase 2 trial assessed the antitumor activity of RO4929097, a gamma-secretase inhibitor of Notch signaling, with respect to the progression-free and overall survival of patients with
Giulia Puliatti et al.
Progress in neurobiology, 227, 102482-102482 (2023-06-16)
Several studies including ours reported the detrimental effects of extracellular tau oligomers (ex-oTau) on glutamatergic synaptic transmission and plasticity. Astrocytes greatly internalize ex-oTau whose intracellular accumulation alters neuro/gliotransmitter handling thereby negatively affecting synaptic function. Both amyloid precursor protein (APP) and
Lukas P Feilen et al.
eLife, 11 (2022-05-18)
Cleavage of membrane proteins in the lipid bilayer by intramembrane proteases is crucial for health and disease. Although different lipid environments can potently modulate their activity, how this is linked to their structural dynamics is unclear. Here, we show that
Edgar Dawkins et al.
The Journal of biological chemistry, 299(4), 103027-103027 (2023-02-23)
Imbalances in the amounts of amyloid-β peptides (Aβ) generated by the membrane proteases β- and γ-secretase are considered as a trigger of Alzheimer's disease (AD). Cell-free studies of γ-secretase have shown that increasing membrane thickness modulates Aβ generation but it
Enzyme-substrate interface targeting by imidazole-based I?-secretase modulators activates I?-secretase and stabilizes its interaction with APP.
Petit, et al.
The Embo Journal, 41, e111084-e111084 (2022)
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