911798
N-(4-Bromophenyl)-N-phenylacrylamide
≥95%
Synonym(s):
Electrophilic scout fragment, KB05, Scout fragment for targetable cysteine
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Application
N-(4-Bromophenyl)-N-phenylacrylamide is a cysteine-reactive small-molecule fragment for chemoproteomic and ligandability studies for both traditionally druggable proteins as well as ″undruggable,″ or difficult-to-target, proteins. This fragment electrophile, or ″scout″ fragment, can be used alone in fragment-based covalent ligand discovery or incorporated into bifunctional tools such as electrophilic PROTAC® molecules for targeted protein degradation as demonstrated by the Cravatt Lab for E3 ligase discovery.
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Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
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Product No.
Description
Pricing
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
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Nature, 534(7608), 570-574 (2016-06-17)
Small molecules are powerful tools for investigating protein function and can serve as leads for new therapeutics. Most human proteins, however, lack small-molecule ligands, and entire protein classes are considered 'undruggable'. Fragment-based ligand discovery can identify small-molecule probes for proteins
Nature chemical biology, 15(7), 737-746 (2019-06-19)
Ligand-dependent protein degradation has emerged as a compelling strategy to pharmacologically control the protein content of cells. So far, however, only a limited number of E3 ligases have been found to support this process. Here, we use a chemical proteomic
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