910538

(S,R,S)-AHPC-PEG₂-butyl alkyne

≥95%

• Sinônimo(s): (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
• Fórmula empírica (Notação de Hill): C₃₄H₄₈N₄O₆S
• Peso molecular: 640.83
• Código UNSPSC: 51171641

Propriedades

• ligand: VH032
• Ensaio: ≥95%
• Formulário: (Liquid or Semi-solid or Paste or Solid)
• adequação da reação: reaction type: click chemistry; reagent type: ligand-linker conjugate
• grupo funcional: alkyne
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres 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)COCCOCCCCCCC#C

Descrição

Aplicação

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.

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 12 - Non Combustible Liquids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable