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565771

γ-Secretase Inhibitor X

Name: &#947;-Secretase Inhibitor X
Brand: MM

≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem^®

同義詞:

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

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經驗公式（希爾表示法）:

C₃₉H₅₂N₄O₆

分子量：:

672.85

UNSPSC Code:

12352200

NACRES:

NA.54

Assay:

≥90% (HPLC)

Form:

liquid

Storage condition:

OK to freeze, desiccated, protect from light

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屬性

產品名稱

γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM

Quality Segment

100

assay

≥90% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, desiccated, protect from light

shipped in

ambient

storage temp.

−20°C

描述

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
Aβ_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)

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本產品	565750	565763	565794
Sigma-Aldrich 565771 γ-Secretase Inhibitor X	Sigma-Aldrich 565750 γ-Secretase Inhibitor I	Sigma-Aldrich 565763 γ-Secretase Inhibitor VI	Sigma-Aldrich 565794 β-Secretase Inhibitor IV
description InSolution, ≥90%, 1 mM	description The γ-Secretase Inhibitor I controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.	description The γ-Secretase Inhibitor VI, also referenced under CAS 287196-57-0, controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.	description InSolution, ≥95%
form liquid	form solid	form solid	form liquid
assay ≥90% (HPLC)	assay ≥90% (HPLC)	assay ≥98% (HPLC)	assay ≥95% (HPLC)
manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®
Quality Level 100	Quality Level 200	Quality Level 100	Quality Level 100
storage temp. −20°C	storage temp. −20°C	storage temp. −20°C	storage temp. −70°C
storage condition protect from light, OK to freeze, desiccated	storage condition desiccated (hygroscopic), OK to freeze	storage condition OK to freeze	storage condition avoid repeated freeze/thaw cycles, protect from light, desiccated (hygroscopic), OK to freeze

存儲類別/等級

10 - Combustible liquids

到底發生了什麼事？

WGK 1

閃點 (F)

188.6 °F - closed cup - (Dimethylsulfoxide)

閃點（°C）

87 °C - closed cup - (Dimethylsulfoxide)

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γ-Secretase Inhibitor X

≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem^®