E7820-C₃-NH₂ hydrochloride

C₂₀H₂₁N₅O₃S · xHCl

411.48 (free base basis)

Protein degrader building block E7820-C₃-NH₂ hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC^® (proteolysis-targeting chimeras) research. This conjugate contains a DCAF15-recruiting ligand E7820 (SML2950), an alkyl 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 degrader, 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 degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Protein Degrader Building Blocks

Technology Spotlight: DCAF15 Degrader Building Blocks for Targeted Protein Degradation

In vivo target protein degradation induced by PROTACs based on E3 ligase DCAF15

E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones

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

100

2-8℃