추천 제품
ligand
VH032 derivative
형태
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
애플리케이션
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.
기타 정보
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.
관련 제품
제품 번호
설명
가격
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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