913162
Enantioprobe (R)-5
≥95%
Synonym(s):
(R)-N-(1-Benzylpyrrolidin-3-yl)-3-(3-(but-3-yn-1-yl)-3H-diazirin-3-yl)-N-methylpropanamide, Fully functionalized enantioprobe, Ligandability probe
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About This Item
Empirical Formula (Hill Notation):
C20H26N4O
Molecular Weight:
338.45
UNSPSC Code:
12161600
Assay
≥95%
form
liquid
storage temp.
−20°C
Application
Enantioprobe (R)-5 is one of 16 fully functionalized, enantiomeric fragment probes developed in the Cravatt. 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 (R)-5′s paired fragment is available as Enantioprobe (S)-5 (cat# 912689).
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
related product
Product No.
Description
Pricing
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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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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