Pomalidomide-benzyl-piperazine hydrochloride

C₂₅H₂₅N₅O₅ · xHCl

475.50 (free base basis)

Protein degrader building block Pomalidomide-benzyl-piperazine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a rigid linker, 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 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 Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

100

2-8℃

O=C(N(C1CCC(NC1=O)=O)C2=O)C3=C2C=CC=C3NC(C4=CC=C(CN5CCNCC5)C=C4)=O.Cl