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S4562

Sigma-Aldrich

β-Secretase inhibitor

≥97% (HPLC), powder

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About This Item

Formule empirique (notation de Hill):
C73H118N16O27
Poids moléculaire :
1651.81
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Source biologique

synthetic (organic)

Niveau de qualité

Pureté

≥97% (HPLC)

Forme

powder

Poids mol.

~_1.65 kDa

Couleur

white

Pf

200 °C

Solubilité

DMSO: soluble

Conditions d'expédition

dry ice

Température de stockage

−20°C

Amino Acid Sequence

Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe

Description générale

β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1), an aspartic protease belongs to the protease family of enzymes comprises of six luminal cysteine residues. These residues help in the formation of three intermolecular disulfide bonds and N-linked glycosylation sites.

Application

β-Secretase inhibitor has been used as β-site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) inhibitor in BACE1 inhibitor assay.(2)
β-Secretase inhibitor may be used to inhibit BACE1 in studies related to AD.

Actions biochimiques/physiologiques

β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) is a β-secretase that initiates the production of amyloid protein in Alzheimer′s dieases (AD) patients. β-Secretase inhibitors decrease the generation of β amyloid and formation of amyloid plaques typical of AD.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)


Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Jungmi Lee et al.
Analytica chimica acta, 1022, 89-95 (2018-05-08)
Amyloid-β (Aβ) is generated by proteolytic processing of amyloid precursor protein (APP) by beta-secretase (BACE-1) and gamma-secretase. Amyloid-β is responsible for the formation of senile plaques in Alzheimer's disease (AD). Consequently, inhibition of β-secretase (BACE-1), a rate-limiting enzyme in the
Hans Hilpert et al.
Journal of medicinal chemistry, 56(10), 3980-3995 (2013-04-18)
An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and highly brain penetrant BACE1
beta-secretase inhibitor; a promising novel therapeutic drug in Alzheimer?s disease
Menting KW, et al.
Frontiers in Aging Neuroscience, 6, 165-165 (2014)
S Sinha et al.
Nature, 402(6761), 537-540 (1999-12-11)
Proteolytic processing of the amyloid precursor protein (APP) generates amyloid beta (Abeta) peptide, which is thought to be causal for the pathology and subsequent cognitive decline in Alzheimer's disease. Cleavage by beta-secretase at the amino terminus of the Abeta peptide
Patty C Kandalepas et al.
Acta neuropathologica, 126(3), 329-352 (2013-07-04)
β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) is the β-secretase that initiates Aβ production in Alzheimer's disease (AD). BACE1 levels are increased in AD, which could contribute to pathogenesis, yet the mechanism of BACE1 elevation is unclear. Furthermore, the

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