910538

(S,R,S)-AHPC-PEG₂-butyl alkyne

≥95%

• 别名: (2S,4R)-1-((S)-3,3-Dimethyl-2-(2-(2-(oct-7-yn-1-yloxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, (S,R,S)-AHPC-2-2-6-alkyne, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• 经验公式（希尔记法）: C₃₄H₄₈N₄O₆S
• 分子量: 640.83
• 分類程式碼代碼: 51171641

属性

• ligand: VH032
• 化驗: ≥95%
• 形狀: (Liquid or Semi-solid or Paste or Solid)
• 反應適用性: reaction type: click chemistry; reagent type: ligand-linker conjugate
• 官能基: alkyne
• 儲存溫度: 2-8°C
• SMILES 字串: O=C(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)COCCOCCCCCCC#C

说明

應用

Protein degrader builiding block (S,R,S)-AHPC-PEG₂-butyl alkyne 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 alkyne for click chemistry with an azide 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 pendant alkyne group, 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

法律資訊

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

安全信息

• 儲存類別代碼: 12 - Non Combustible Liquids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable