912417
Enantioprobe (S)-1
≥95%
Sinônimo(s):
(S)-3-(3-(But-3-yn-1-yl)-3H-diazirin-3-yl)-1-(2-phenylpyrrolidin-1-yl)propan-1-one, Fully functionalized enantioprobe, Ligandability probe
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About This Item
Fórmula empírica (Notação de Hill):
C18H21N3O
Número CAS:
Peso molecular:
295.38
Código UNSPSC:
12161600
Ensaio
≥95%
forma
powder
temperatura de armazenamento
−20°C
Aplicação
Enantioprobe (S)-1 is one of 16 fully functionalized, enantiomeric fragment probes developed in the Cravatt lab. Combining fragment-based ligand discovery (FBLD) with chemical proteomics, the enantioprobe library assesses ligandability across proteomes. Each enantioprobe contains a structurally variable fragment for interaction with proteins, photoactivatable diazirine for UV-induced covalent protein labeling, and bioorthogonal alkyne handle for detection, enrichment, and identification. Of the eight enantiomeric pairs, each differs by one stereocenter, and comparing stereoselective fragment-protein interactions between the pairs simplifies validation of authentic protein-binding events. Enantioprobe (S)-1′s paired fragment is available as Enantioprobe (R)-1 (cat# 912905).
Together, the 16 enantioprobes support ligandability studies in living cells, a significant method for development of chemical probes and lead discovery efforts to find binders for traditionally ″undruggable″ protein targets. This strategy is also compatible with multiplexing for higher throughput.
Together, the 16 enantioprobes support ligandability studies in living cells, a significant method for development of chemical probes and lead discovery efforts to find binders for traditionally ″undruggable″ protein targets. This strategy is also compatible with multiplexing for higher throughput.
Supporting reagents:
- Fluorophore-conjugated azide tags for SDS-PAGE in-gel profiling: 910147, 760757, 760765, 777315, 777323
- Azide-biotin tags for enrichment: 901765, 914134, 914460, 762024, 900912, 900891, QBD10825)
- Azide capture solid supports: 900957, 742627
- Streptavidin for biotin enrichment: S6940, E5529, E2513, 69203, 16-126, S1638
- Mass spectrometry and Multiplexing
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Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
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Yujia Wang et al.
Nature chemistry, 11(12), 1113-1123 (2019-10-30)
A fundamental challenge in chemical biology and medicine is to understand and expand the fraction of the human proteome that can be targeted by small molecules. We recently described a strategy that integrates fragment-based ligand discovery with chemical proteomics to
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