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925004

Sigma-Aldrich

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

ligand

E7820

Quality Level

100

reaction suitability

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

functional group

amine

storage temp.

2-8°C

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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

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

related product

Product No.
Description
Pricing

SML2950

E7820, ≥98% (HPLC)

Storage Class Code

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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