912689

Sigma-Aldrich

Enantioprobe (S)-5

≥95%

别名:
(S)-N-(1-Benzylpyrrolidin-3-yl)-3-(3-(but-3-yn-1-yl)-3H-diazirin-3-yl)-N-methylpropanamide, Ligandability probe, Fully functionalized enantioprobe
Empirical Formula (Hill Notation):
C20H26N4O
分子量:
338.45

Quality Level

assay

≥95%

form

liquid

storage temp.

−20°C

Application

Enantioprobe (S)-5 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)-5′s paired fragment is available as Enantioprobe (R)-5 (cat# 913162).
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
  • WGK Germany

    WGK 3

    Flash Point(F)

    Not applicable

    Flash Point(C)

    Not applicable

    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...
    技术文章
    Ligandability describes the propensity of a protein target to bind a small molecule with high affinity. It is a precursor to evaluating druggability, which requires more advanced translational pharmacological effects and drug-like properties in vivo.
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