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911798 Sigma-Aldrich

N-(4-Bromophenyl)-N-phenylacrylamide

≥95%

Synonym: Electrophilic scout fragment, KB05, Scout fragment for targetable cysteine

  • CAS Number 1956368-15-2

  • Empirical Formula (Hill Notation) C15H12BrNO

  • Molecular Weight 302.17

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Properties

Related Categories Chemical Biology, Chemical Synthesis, Probes and Sensors, Scout Fragments for Lead Discovery
Quality Level   100
assay   ≥95%
form   (Powder or crystals or solid or chunks)
storage temp.   2-8°C

Description

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.

Other Notes

Technology Spotlight: Proteomic Ligandability Assessment

Proteome-wide covalent ligand discovery in native biological systems

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

Legal Information

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

Safety & Documentation

Safety Information

WGK Germany 
WGK 3

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Proteomic Ligandability Assessment

Ligandability describes the propensity of a protein target to bind a small molecule with high affinity. It is a precursor to evaluating druggability, which requires more advanced translational pharma...
Keywords: Cancer, Catalysis, Cell culture, Drug discovery, Ligands, Mass spectrometry, Proteomics, Transcription

Peer-Reviewed Papers
15

References

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