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Safety Information

CS0010

Sigma-Aldrich

β-Secretase (BACE1) Activity Detection Kit (Fluorescent)

1 kit sufficient for 250 reactions

Synonym(s):

BACE1 Activity Detection Kit (Fluorescent)

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About This Item

UNSPSC Code:
12161503
NACRES:
NA.84

Quality Level

usage

 kit sufficient for 250 reactions

shipped in

wet ice

storage temp.

−20°C

Gene Information

human ... BACE1(23621)

Biochem/physiol Actions

BACE1 is a transmembrane protease responsible for the β site cleavage of the amyloid precursor protein (APP) to produce amyloid β peptide (Aβ). The accumulation of Aβ in the brain is a primary cause for the progression of Alzheimer′s. BACE1 is a target for inhibitor drug discovery.

Suitability

The kit provides all the reagents required for an efficient detection of BACE1 activity. It contains an enzyme to be used for screening for potential BACE1 inhibitors. The assay is based on the fluorescence resonance energy transfer (FRET) method in which the fluorescence signal enhancement is observed after substrate cleavage by BACE1.

Kit Components Only

Product No.
Description

  • Fluorescent Assay Buffer 50 mL

  • Stop Solution 15 mL

  • Substrate (MOCA-SEV-NL-DAEFR-DNP-RR) 500 μL

  • Assay Standard 140 μL

  • BACE1 (β−Secretase) 300 units 100 μL

Storage Class Code

10 - Combustible liquids

Regulatory Information

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Lucas J Gutiérrez et al.
Journal of biomolecular structure & dynamics, 37(1), 229-246 (2018-01-06)
We report in this work new substituted aminopyrimidine derivatives acting as inhibitors of the catalytic site of BACE1. These compounds were obtained from a molecular modeling study. The theoretical and experimental study reported here was carried out in several steps:
Piyoosh Sharma et al.
European journal of medicinal chemistry, 167, 510-524 (2019-02-21)
The multitarget-directed strategy offers an effective and promising paradigm to treat the complex neurodegenerative disorder, such as Alzheimer's disease (AD). Herein, a series of N-benzylpiperidine analogs (17-31 and 32-46) were designed and synthesized as multi-functional inhibitors of acetylcholinesterase (AChE) and
Maricarmen Hernández-Rodríguez et al.
Molecular neurobiology, 57(9), 3979-3988 (2020-07-09)
The increase of amyloid beta (Aβ) release and hyperphosphorylation of Tau protein represents the main events related to Alzheimer's disease (AD). Furthermore, the sporadic type represents the most common form of AD. Therefore, the establishment of a non-transgenic animal model
Fluoro-benzimidazole derivatives to cure Alzheimer's disease: In-silico studies, synthesis, structure-activity relationship and in vivo evaluation for β secretase enzyme inhibition.
Sayyad Ali et al.
Bioorganic chemistry, 88, 102936-102936 (2019-05-06)
Piyoosh Sharma et al.
ACS chemical neuroscience, 10(10), 4361-4384 (2019-09-07)
Multitargeted hybrids of N-benzylpiperidine and substituted 5-phenyl-1,3,4-oxadiazoles were designed, synthesized, and evaluated against Alzheimer's disease (AD). Tested compounds exhibited moderate to excellent inhibition against human acetylcholinesterase (hAChE), butyrylcholinesterase (hBChE), and beta-secretase-1 (hBACE-1). The potential leads 6g and 10f exhibited balanced

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