565755
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.
Synonym(s):
γ-Secretase Inhibitor II, MW167
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About This Item
Empirical Formula (Hill Notation):
C33H57F2N5O9
Molecular Weight:
705.83
UNSPSC Code:
12352200
NACRES:
NA.54
Recommended Products
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.
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
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.
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
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (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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