128886-88-4Relevant articles and documents
Photo-crosslinking of clinically relevant kinases using H89-derived photo-affinity probes
Stolze, Sara C.,Liu, Nora,Wijdeven, Ruud H.,Tuin, Adriaan W.,Van Den Nieuwendijk, Adrianus M. C. H.,Florea, Bogdan I.,Van Der Stelt, Mario,Van Der Marel, Gijsbert A.,Neefjes, Jacques J.,Overkleeft, Herman S.
, p. 1809 - 1817 (2016)
The profiling of kinases using established proteomics techniques is hampered by their non-covalent mode-of-action. One way to overcome this caveat is the use of probes featuring photo-labelling groups that can be activated by UV irradiation to generate a reactive species that will establish a covalent bond to the enzyme. In this study we have used the well-known kinase inhibitor H89 as a lead for the development of probes for the affinity-based profiling of clinically relevant kinases. A labelling protocol was established for recombinant kinases and more complex protein mixtures using gel-based techniques. We also show that the probes act in a competitive manner with other kinase inhibitors.
CARBENE MASS TAGGING
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Page/Page column 20-22, (2020/12/07)
The disclosure relates to a diazirine precursor mass tag compound represented by structural formula (I). Also disclosed is a method for detecting analytes in a sample, comprising derivatizing the analytes with the compound of formula (I), and detecting th
A new cleavable carbene-generating reagent with 3-phenyl-3-trifluoromethyldiazirine photophore
Kempin, Uwe,Kanaoka, Yuichi,Hatanaka, Yasumam
, p. 465 - 468 (2007/10/03)
Synthesis of a 3-phenyl-3-trifluoromethyldiazirine derivative having a cleavable 1,2-diol moiety for photocross-linking technique is described. An ester of cinnamic acid derivative was prepared by the Wittig reaction of 2-methoxy-4-[3-trifluoromethyl-3H-diazirin-3-yl]benzaldehyde which can be readily prepared by the Friedel-Crafts reaction of corresponding phenyldiazirine. The osmium oxidation of the olefinic bond gave the desired diol derivative, ethyl 2,3-dihydroxy-3-[2-methoxy-4-(3-trifluoromethyl-3H-diazirin-3-yl)phenyl] propionate, in a high yield. The cleavability of the diol group was confirmed by the conventional periodate oxidation to give the starting aldehyde.
