925004
E7820-PEG1-NH2 hydrochloride
Synonym(s):
N-(2-(2-Aminoethoxy)ethyl)-3-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzamide, Crosslinker−E3 Ligase ligand conjugate hydrochloride, DCAF15 protein degrader building block
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About This Item
Empirical Formula (Hill Notation):
C21H23N5O4S · xHCl
Molecular Weight:
441.50 (free base basis)
NACRES:
NA.22
UNSPSC Code:
12352200
ligand
E7820
reaction suitability
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
functional group
amine
storage temp.
2-8°C
Quality Level
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Application
Protein degrader building block E7820-PEG1-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
Protein Degrader Building Blocks
Technology Spotlight: DCAF15 Degrader Building Blocks for Targeted Protein Degradation
Other Notes
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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In vivo target protein degradation induced by PROTACs based on E3 ligase DCAF15.
Liang Li et al.
Signal transduction and targeted therapy, 5(1), 129-129 (2020-07-28)
Tasuku Ishida et al.
SLAS discovery : advancing life sciences R & D, 26(4), 484-502 (2020-11-05)
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to
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