Pomalidomide-dipiperazine-NH₂ hydrochloride, 1 X 50 mg (915572-50MG)

Protein degrader building block Pomalidomide-dipiperazine-NH₂ 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 an acid on the target warhead. 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 terminal 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

Read Less