Lim, Bumhee; Lee, Jinah; Kim, Byungjin; Lee, Rang; Park, Jaehyun; Oh, Dong-Chan; Gam, Jongsik; Lee, Jeeyeon published the artcile< Target Identification of a 1,3,4-Oxadiazin-5(6H)-One Anticancer Agent via Photoaffinity Labelling>, Application In Synthesis of 25055-82-7, the main research area is oxadiazinone protein anticancer agent photoaffinity labeling probe.
Rational design and synthetic feasibility are critical factors for the photoaffinity labeling (PAL) approach, which can identify protein targets of bioactive small mols. under native cellular conditions. In this study, we developed photoaffinity labeling probes derived from 1,3,4-oxadiazin-5(6H)-ones (OPALs) for LL-2003, a previously reported potential anticancer agent against IGF-1R and Src. Our photoaffinity labeling strategy enabled successful photo-crosslinking of the probes (OPAL-6 and OPAL-8) with the target proteins in both mammalian cell lysates and live MCF7, A549, HepG2 and HeLa cells in situ. In vitro and in situ labeling demonstrated different patterns and expression levels of the proteome, and the strongest band for Src appeared in the A549 cell line. An in-gel fluorescence scan combined with MS/MS anal. of the IGF-1R overexpressed insect proteome labeled by OPAL-6 and OPAL-8 identified the binding location of the synthesized probes.
Asian Journal of Organic Chemistry published new progress about Antitumor agents. 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Application In Synthesis of 25055-82-7.
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