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Sigma-Aldrich

γ-Secretase Inhibitor II

The γ-Secretase Inhibitor II controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.

Sinónimos:

γ-Secretase Inhibitor II, MW167

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About This Item

Fórmula empírica (notación de Hill):
C33H57F2N5O9
Peso molecular:
705.83
UNSPSC Code:
12352200
NACRES:
NA.54

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

white

solubility

DMSO: 10 mM

shipped in

ambient

storage temp.

−20°C

General description

A cell-permeable, reversible and selective peptidomimetic inhibitor of γ-secretase (IC50 = 13 µM for Aβ). Displays only weak inhibitory activity against calpain II (IC50 = 100 µM in a purified enzyme assay).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, reversible and selective peptidomimetic inhibitor of γ-secretase with an IC50 of 13 µM for the inhibition of amyloid β-protein (Aβ) production in β-amyloid precursor protein (APP)-transfected Chinese hamster ovary cells. Displays only weak inhibitory activity against calpain II (IC50 = 100 µM in a purified enzyme assay).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
γ-secretase
Product does not compete with ATP.
Reversible: yes
Target IC50: 13 µM against γ-secretase

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wolfe, M.S., et al. 1999. Biochemistry38, 4720.
Wolfe, M.S., et al. 1998. J. Med. Chem. 41, 6.
Citron, M., et al. 1996. Proc. Natl. Acad. Sci. USA93, 13170.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

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Yaxiong Yang et al.
Journal of neurochemistry, 88(6), 1361-1372 (2004-03-11)
Glutamate uptake by high affinity glutamate transporters is essential for preventing excitotoxicity and maintaining normal synaptic function. We have discovered a novel role for presenilin-1 (PS1) as a regulator of glutamate transport. PS1-deficient neurons showed a decrease in glutamate uptake

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