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
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A propos de cet article
Formule empirique (notation de Hill) :
C23H28F3N3O3S
Numéro CAS:
Poids moléculaire :
483.55
UNSPSC Code:
12352101
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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
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.
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.
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.
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Guilherme Vieira de Castro et al.
Chemical communications (Cambridge, England), 55(10), 1482-1485 (2019-01-16)
Systematic characterization of a series of fluorinated VHL ligands, varying binding affinity and position of the trifluoromethyl group, qualifies a spy molecule for competitive 19F NMR screening and reveals guiding principles to develop highly sensitive assays with low material consumption.
Carles Galdeano et al.
Journal of medicinal chemistry, 57(20), 8657-8663 (2014-08-29)
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success. The von Hippel-Lindau protein (pVHL) is the substrate recognition subunit of the VHL E3 ligase that targets HIF-1α