909378

(S,R,S)-AHPC-PEG₆-Azide

≥95%

• 別名: (2S,4R)-1-((S)-23-Azido-2-(tert-butyl)-4-oxo-6,9,12,15,18,21-hexaoxa-3-azatricosanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, 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）: C₃₆H₅₅N₇O₁₀S
• CAS番号: 2086298-71-5
• 分子量: 777.93
• MDL番号: MFCD32669901
• UNSPSCコード: 51171641
• NACRES: NA.22

特性

• ligand: VH032
• アッセイ: ≥95%
• フォーム: (Liquid or Semi-Solid or Paste or Solid)
• 反応適合性: reaction type: click chemistry; reagent type: ligand-linker conjugate
• 官能基: azide
• 保管温度: 2-8°C
• SMILES記法: O=C(COCCOCCOCCOCCOCCOCCN=[N+]=[N-])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
• InChI: 1S/C36H55N7O10S/c1-26-32(54-25-39-26)28-7-5-27(6-8-28)22-38-34(46)30-21-29(44)23-43(30)35(47)33(36(2,3)4)41-31(45)24-53-20-19-52-18-17-51-16-15-50-14-13-49-12-11-48-10-9-40-42-37/h5-8,25,29-30,33,44H,9-24H2,1-4H3,(H,38,46)(H,41,45)/t29-,30+,33-/m1/s1
• InChI Key: AJSBEOXYBAZQFR-YLJHYDRVSA-N

詳細

アプリケーション

Protein degrader builiding block (S,R,S)-AHPC-PEG₆-Azide 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 azide for click chemistry with an alkyne 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 azide group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

その他情報

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