Synonyms: (2S,4R)-1-((S)-2-(tert-Butyl)-4-oxo-7,10,13,16,19,22-hexaoxa-3-azapentacos-24-ynoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide; Crosslinker-E3 Ligase ligand conjugate; Protein degrader building block for PROTAC(R) research; Template for synthesis of targeted protein degrader; VH032 conjugate
Molecular Formula: C38H56N4O10S
Molecular Weight: 760.94
Linear Structural Formula: C38H56N4O10S
Storage: 2-8C
Application: Protein degrader builiding block (S,R,S)-AHPC-PEG6-Alkyne enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant alkyne for click chemistry with an azide 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 alkyne group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Legal Information: PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
Other Notes: Technology Spotlight: Degrader Building Blocks for Targeted Protein DegradationPortal: Building PROTAC(R) 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 PROTACs