909416

Fluorinated VHL spy molecule 1

• Synonyma: (2S,4R)-1-(3,3-Dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)-3-(trifluoromethyl)benzyl)pyrrolidine-2-carboxamide
• Empirický vzorec (Hillův zápis): C₂₃H₂₈F₃N₃O₃S
• Číslo CAS: 2290526-08-6
• Molekulová hmotnost: 483.55
• UNSPSC Code: 12352101

Vlastnosti

• ligand: VH032 derivative
• form: solid
• SMILES string: 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

Popis

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.

Other Notes

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.

Bezpečnostní informace

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable