909262

(S,R,S)-AHPC-PEG₄-Azide

≥95%

• Synonyme(s) : (2S,4R)-1-((S)-17-Azido-2-(tert-butyl)-4-oxo-6,9,12,15-tetraoxa-3-azaheptadecanoyl)-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
• Formule empirique (notation de Hill): C₃₂H₄₇N₇O₈S
• Numéro CAS: 1797406-81-5
• Poids moléculaire : 689.82
• Code UNSPSC : 51171641

Propriétés

• ligand: VH032
• Pureté: ≥95%
• Forme: liquid
• Capacité de réaction: reaction type: click chemistry
• Pertinence de la réaction: reagent type: ligand-linker conjugate
• Groupe fonctionnel: azide
• Température de stockage: 2-8°C
• Chaîne SMILES: O=C(COCCOCCOCCOCCN=[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

Description

Application

Protein degrader builiding block (S,R,S)-AHPC-PEG₄-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.

Autres remarques

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 Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

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: 10 - Combustible liquids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable