910546

(S,R,S)-AHPC-C₆-PEG₃-butyl alkyne

≥95%

• Synonyme(s) : (2S,4R)-1-((S)-2-(tert-Butyl)-4-oxo-10,13,16-trioxa-3-azatetracos-23-ynoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, (S,R,S)-AHPC-6-2-2-6-alkyne, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader, VH032 conjugate
• Formule empirique (notation de Hill): C₄₀H₆₀N₄O₇S
• Poids moléculaire : 740.99
• Code UNSPSC : 12352101

Propriétés

• ligand: VH032
• Pureté: ≥95%
• Forme: (Liquid or Semi-Solid or Paste or Solid)
• Capacité de réaction: reaction type: click chemistry
• Pertinence de la réaction: reagent type: ligand-linker conjugate
• Groupe fonctionnel: alkyne
• Température de stockage: 2-8°C
• Chaîne SMILES: 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)CCCCCOCCOCCOCCCCCCC#C

Description

Application

Protein degrader builiding block (S,R,S)-AHPC-C₆-PEG₃-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.

Autres remarques

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 12 - Non Combustible Liquids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable