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反應適用性
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
品質等級
官能基
amine
儲存溫度
2-8°C
SMILES 字串
O=C1C(N2C(C(C=CC=C3N4CCN(C(C5CCNCC5)=O)CC4)=C3C2=O)=O)CCC(N1)=O.Cl
應用
Protein degrader building block Pomalidomide-piperazine-piperidine-4-carboxamide hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, a rigid 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.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
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其他說明
法律資訊
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
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产品编号
说明
价格
訊號詞
Danger
危險聲明
危險分類
Repr. 1B
儲存類別代碼
6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
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