Synonyms: 2-(2-Aminoethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)acetamide hydrochloride; C5 Lenalidomide conjugate; Crosslinker-E3 Ligase ligand conjugate; Protein degrader building block for PROTAC(R) research; Template for synthesis of targeted protein degrader
Molecular Formula: C17H20N4O5 · xHCl
Linear Structural Formula: C17H20N4O5 · xHCl
Purity: >=95%
Storage: 2-8C
Application: Protein degrader builiding block C5 Lenalidomide-PEG1-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 with alternative exit vector and a PEGylated crosslinker with pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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.
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 Discovery