909416

Fluorinated VHL spy molecule 1

• Synonyme(s) : (2S,4R)-1-(3,3-Dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)-3-(trifluoromethyl)benzyl)pyrrolidine-2-carboxamide
• Formule empirique (notation de Hill): C₂₃H₂₈F₃N₃O₃S
• Numéro CAS: 2290526-08-6
• Poids moléculaire : 483.55
• Code UNSPSC : 12352101

Propriétés

• ligand: VH032 derivative
• Forme: solid
• Chaîne SMILES: O=C([C@@H]1C[C@@H](O)CN1C(CC(C)(C)C)=O)NCC2=CC=C(C3=C(C)N=CS3)C(C(F)(F)F)=C2

Description

Application

Fluorinated VHL Spy Molecule 1 can be used for the discovery of new von Hippel-Lindau (VHL) binders. Based on VH032 (cat# 901490), this reporter was designed in the lab of Alessio Ciulli to bind the hydroxyproline (Hyp) recognition site of VHL. When used in competition ligand-observed 19F NMR screening experiments, its displacement indicates binding by another molecule. Additional Fluorinated VHL Spy Molecules are available as listings 909432, 909440 and 909459.
The E3 ligase VHL is of growing interest for targeted protein degradation, and these spy molecules will facilitate the identification of novel VHL ligands and VHL-based degraders.

Autres remarques

Spy vs. spy: selecting the best reporter for 19F NMR competition experiments

Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable