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Merck
CN

924997

Sigma-Aldrich

E7820-C9-NH2 hydrochloride

别名:

N-(9-Aminononyl)-3-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, DCAF15 protein degrader building block

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About This Item

经验公式(希尔记法):
C26H33N5O3S · xHCl
分子量:
495.64 (free base basis)
NACRES:
NA.22

ligand

E7820

质量水平

反应适用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能团

amine

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应用

Protein degrader building block E7820-C9-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

法律信息

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

相关产品

产品编号
说明
价格

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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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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