919489
CCW16-C6-PEG3-butyl-BocNH
别名:
tert-butyl (6-(2-(2-((6-(4-(4-(N-Benzyl-2-chloroacetamido)phenoxy)phenoxy)hexyl)oxy)ethoxy)ethoxy)hexyl)carbamate, Crosslinker-E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, RNF4-targeting building block, Template for synthesis of targeted protein degrader
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About This Item
推荐产品
ligand
CCW16
品質等級
形狀
viscous liquid
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=C(CCl)N(CC1=CC=CC=C1)C2=CC=C(C=C2)OC3=CC=C(OCCCCCCOCCOCCOCCCCCCNC(OC(C)(C)C)=O)C=C3
應用
Protein degrader building block CCW16-C6-PEG3-butyl-BocNH enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a RING finger protein 4 (RNF4)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, 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
Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications
Targeted Protein Degradation by Small Molecules
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications
Targeted Protein Degradation by Small Molecules
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
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
10 - Combustible liquids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
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