905399

(S,R,S)-AHPC-PEG₂-butyl chloride

• 別名: (2S,4R)-1-((S)-2-(2-(2-((6-Chlorohexyl)oxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, (S,R,S)-AHPC-2-2-6-Cl, Crosslinker−E3 ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• 実験式（ヒル表記法）: C₃₂H₄₇ClN₄O₆S
• CAS番号: 1835705-57-1
• 分子量: 651.26
• MDL番号: MFCD31560480
• UNSPSCコード: 12352101
• NACRES: NA.22

特性

• ligand: VH032
• アッセイ: ≥95%
• 形状: liquid
• 反応適合性: reactivity: sulfuryl reactive; reagent type: ligand-linker conjugate
• 官能基: alkyl halide
• 保管温度: 2-8°C
• SMILES記法: ClCCCCCCOCCOCC(N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C)=O

詳細

アプリケーション

Protein degrader builiding block (S,R,S)-AHPC-PEG₂-Butyl Chloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant chloroalkane for reactivity with a nucleophilic group on a 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 pendant chloro group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

その他情報

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

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

法的情報

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

安全性情報

• 保管分類コード: 10 - Combustible liquids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable