565771
γ-Secretase Inhibitor X
≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem®
Sinonimo/i:
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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Informazioni su questo articolo
Formula empirica (notazione di Hill):
C39H52N4O6
Peso molecolare:
672.85
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥90% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, desiccated, protect from light
Servizio Tecnico
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Permettici di aiutartiNome del prodotto
γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
Quality Level
assay
≥90% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated, protect from light
shipped in
ambient
storage temp.
−20°C
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
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
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.
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)
Classe di stoccaggio
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Certificati d'analisi (COA)
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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
Numero articolo commerciale globale
| SKU | GTIN |
|---|---|
| 565771-250UG | 04055977267839 |
| 565771-500UG | 04055977267846 |