ligand
E7820
质量水平
反应适用性
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
官能团
amine
储存温度
2-8°C
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应用
Protein degrader building block E7820-C3-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
Protein Degrader Building Blocks
Technology Spotlight: DCAF15 Degrader Building Blocks for Targeted Protein Degradation
其他说明
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
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
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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