918350
C5 Lenalidomide-alkyne-piperidine hydrochloride
≥95%
别名:
N-(2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-3-(piperidin-4-yl)propiolamide hydrochloride, Crosslinker-E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader
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About This Item
经验公式（希尔记法）:
C21H22N4O4 · xHCl
分子量:
394.42 (free base basis)
推荐产品
ligand
C5 Lenalidomide
化驗
≥95%
形狀
powder or crystals
反應適用性
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
官能基
amine
儲存溫度
2-8°C
SMILES 字串
O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(C#CC4CCNCC4)=O)=CC=C31.Cl
應用
Protein degrader building block C5 Lenalidomide-alkyne-piperidine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector, a linker with added rigidity, 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 PROTAC, 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 PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
其他說明
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
法律資訊
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
相關產品
产品编号
说明
价格
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Daniel P Bondeson et al.
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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