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MilliporeSigma Sigma Organics products encompass a wide range of quality reagents, solvents, catalysts, and building blocks for organic synthesis. From benchtop discovery to process development and scale-up, Sigma Organics solutions are built to meet the needs of synthetic chemists.
Protein degrader building block CCW16-PEG1-BocNH enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a RING finger protein 4 (RNF4)-recruiting ligand, a PEGylated crosslinker, and a pendant amine for reactivity with a carboxylic acid on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.Technology Spotlight: Degrader Building Blocks for Targeted Protein DegradationPortal: Building PROTAC™ Degraders for Targeted Protein DegradationCovalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation ApplicationsTargeted Protein Degradation by Small MoleculesSmall-Molecule PROTACS: New Approaches to Protein DegradationTargeted Protein Degradation: from Chemical Biology to Drug DiscoveryPROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
tert-butyl (6-(2-(2-((6-(4-(4-(N-Benzyl-2-chloroacetamido)phenoxy)phenoxy)hexyl)oxy)ethoxy)ethoxy)hexyl)carbamate; Crosslinker-E3 Ligase ligand conjugate; Protein degrader building block for PROTAC(R) research; RNF4-targeting building block; Template for synthesis of targeted protein degrader
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