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Merck
모든 사진(3)

문서

909459

Sigma-Aldrich

Fluorinated VHL Spy Molecule 4

≥98%

동의어(들):

(2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide

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About This Item

실험식(Hill 표기법):
C15H16BrF3N2O3
CAS Number:
Molecular Weight:
409.20
UNSPSC 코드:
12352101

ligand

VH032 derivative

분석

≥98%

형태

powder

SMILES string

O=C([C@@H]1C[C@@H](O)CN1C(CC(F)(F)F)=O)NCC2=CC=C(Br)C=C2

애플리케이션

Fluorinated VHL Spy Molecule 4 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 909416, 909432, and 909440.
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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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
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.

관련 콘텐츠

The Ciulli group are broadly interested with understanding and exploiting the ligandability of protein-protein interactions (PPIs) and protein surfaces within complex biological systems using chemical and structural cell biology approaches. Current research efforts are directed towards targeting PPIs molecular recognition within protein families of biological and medical relevance within the Ubiquitin and Chromatin systems by developing small molecules that disrupt PPIs and that induce targeted protein degradation (PROTAC®) - as tools to probe biology and leads for drug discovery.

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

고객지원팀으로 연락바랍니다.