565771
γ-Secretase Inhibitor X
≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem®
Synonyme(s) :
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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About This Item
Formule empirique (notation de Hill):
C39H52N4O6
Poids moléculaire :
672.85
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.54
Produits recommandés
product name
γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
Niveau de qualité
Pureté
≥90% (HPLC)
Forme
liquid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
desiccated
protect from light
Conditions d'expédition
ambient
Température de stockage
−20°C
Description générale
A cell-permeable hydroxyethylene dipeptide isostere that acts as a highly specific and a potent inhibitor of γ-secretase (Aβtotal IC50 = 17 nM, Aβ40 IC50 = 48 nM, and Aβ42 IC50 = 67 nM in SHSY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. 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.
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.
Actions biochimiques/physiologiques
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
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Forme physique
A 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C).
Autres remarques
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.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
10 - Combustible liquids
Classe de danger pour l'eau (WGK)
WGK 1
Point d'éclair (°F)
188.6 °F - closed cup - (Dimethylsulfoxide)
Point d'éclair (°C)
87 °C - closed cup - (Dimethylsulfoxide)
Certificats d'analyse (COA)
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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.
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
Nicole L Stott Bond et al.
Biomedicines, 11(1) (2023-01-22)
Lung cancer maintains a relatively small survival rate (~19%) over a 5-year period and up to 80-85% of all lung cancer diagnoses are Non-Small Cell Lung Cancer (NSCLC). To determine whether metformin reduces non-small cell lung cancer (NSCLC) LL/2 cell
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
Edgar Dawkins et al.
The Journal of biological chemistry, 299(4), 103027-103027 (2023-02-23)
Imbalances in the amounts of amyloid-β peptides (Aβ) generated by the membrane proteases β- and γ-secretase are considered as a trigger of Alzheimer's disease (AD). Cell-free studies of γ-secretase have shown that increasing membrane thickness modulates Aβ generation but it
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