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Merck
모든 사진(1)

문서

925004

Sigma-Aldrich

E7820-PEG1-NH2 hydrochloride

동의어(들):

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

실험식(Hill 표기법):
C21H23N5O4S · xHCl
Molecular Weight:
441.50 (free base basis)
NACRES:
NA.22

ligand

E7820

Quality Level

반응 적합성

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

작용기

amine

저장 온도

2-8°C

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애플리케이션

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

법적 정보

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

관련 제품

제품 번호
설명
가격

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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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