γ-Secretase Inhibitor X,250UG,565771-250UGCN,Sigma

销售价: ¥ 4588.20 / 件
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订货号 0BW0961
品牌型号 Sigma 565771-250UGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

General description

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.


Biochem/physiol Actions

Cell permeable: yes
Primary Target
total
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


Packaging

Packaged under inert gas


Physical form

A 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.


Preparation Note

Following initial thaw, aliquot and freeze (-20°C).


Other Notes

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.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Standard Handling (A)


技术参数 Specifications
Quality Segment100
assay≥90% (HPLC)
formliquid
manufacturer/tradenameCalbiochem®
storage conditionprotect from light,OK to freeze,desiccated
shipped inambient
storage temp.−20°C
长度(mm)
宽度(mm)
高度(mm)
重量(kg)
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