E3 ligase Ligand-Linker Conjugates 13

Synonym(s):(2S,4R)-1-((S)-2-(2-(2-(2-Azidoethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;Crosslinker−E3 ligase ligand conjugate;Protein degrader building block for PROTAC research;Template for synthesis of targeted protein degrader;VH032 conjugate

CAS NO.：2010159-45-0
Empirical Formula: C28H39N7O6S
Molecular Weight: 601.72
MDL number: MFCD31807300
Update Date: 2024-11-19 23:02:33

E3 ligase Ligand-Linker Conjugates 13 Structural

What is E3 ligase Ligand-Linker Conjugates 13?

The Uses of E3 ligase Ligand-Linker Conjugates 13

Protein degrader builiding block (S,R,S)-AHPC-PEG2-azide 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 azide for click chemistry with a 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 azide group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.