Synonyms: (2S,4R)-1-((S)-14-Amino-2-(tert-butyl)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride; Crosslinker-E3 Ligase ligand conjugate; Protein degrader building block for PROTAC(R) research; Template for synthesis of targeted protein degrader; VH032 conjugate
Molecular Formula: C30H45N5O7S · xHCl
Linear Structural Formula: C30H45N5O7S · xHCl
Purity: >=95%
Storage: 2-8C
Application: Protein degrader builiding block (S,R,S)-AHPC-PEG3-NH2 (HCl salt) 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 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.
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 DegradationImpact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor ScaffoldsDegradation of the BAF Complex Factor BRD9 by Heterobifunctional LigandsAssessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and DegradationTargeted Protein Degradation by Small MoleculesImpact of linker length on the activity of PROTACs