920835

(S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH₂ hydrochloride

• Synonym(e): (2S,4R)-N-{[2-(3-{4-[5-(3-Aminoprop-1-yn-1-yl)pyridin-2-yl]piperazin-1-yl}propoxy)-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-4-hydroxy-1-[(2S)-3-methyl-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, VHL protein degrader building block for PROTAC^® research
• Empirische Formel (Hill-System): C₄₄H₅₂N₈O₅S · xHCl
• Molekulargewicht: 805.00 (free base basis)

Eigenschaften

• Eignung der Reaktion: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• Qualitätsniveau: 100
• Funktionelle Gruppe: amine
• Lagertemp.: 2-8°C

Beschreibung

Anwendung

Protein degrader building block (S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH₂ hydrochloride 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 with alternative exit vector from the widely used VH032 (901490), a rigid inker, and a pendant amine for reactivity with a carboxylic acid 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Sonstige Hinweise

Targeted Protein Degradation by Small Molecules

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable