925039

E7820-PEG₃-NH₂ hydrochloride

• Synonym(s): N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-3-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzamide hydrochloride, Crosslinker–E3 Ligase ligand conjugate, DCAF15 protein degrader building block
• Empirical Formula (Hill Notation): C₂₅H₃₁N₅O₆S · xHCl
• Molecular Weight: 529.61 (free base basis)
• NACRES: NA.22

Properties

• ligand: E7820
• Quality Level: 100
• form: amorphous powder
• reaction suitability: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• functional group: amine
• storage temp.: 2-8°C

Description

Application

Protein degrader builiding block E7820-PEG3-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 ), a PEG 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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable