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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 builiding block (S,R,S)-AHPC-PEG2-butyl amine (HCl salt) enables the synthesis of molecules for targeted protein degradationand PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant amine for reactivity with a carboxyl group 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 pendant 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 DegradationTargeted Protein Degradation by Small MoleculesSmall-Molecule PROTACS: New Approaches to Protein DegradationTargeted Protein Degradation: from Chemical Biology to Drug DiscoveryImpact of linker length on the activity of PROTACsPROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
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