In 2018,Jiang, Fen; Guo, An-ping; Xu, Jia-chen; You, Qi-Dong; Xu, Xiao-Li published 《Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis》.Journal of Medicinal Chemistry published the findings.Product Details of 27489-62-9 The information in the text is summarized as follows:
As the endoplasmic reticulum paralog of Hsp90, Grp94 chaperones a small set of client proteins associated with some diseases, including cancer, primary open-angle glaucoma, and inflammatory disorders. Grp94-selective inhibition has been a potential therapeutic strategy for these diseases. In this study, inspired by the conclusion that ligand-induced “”Phe199 shift”” effect is the structural basis of Grp94-selective inhibition, a series of novel Grp94 selective inhibitors incorporating “”benzamide”” moiety were developed, among which compound I manifested the most potent Grp94 inhibitory activity with an IC50 value of 2 nM and over 1000-fold selectivity to Grp94 against Hsp90α. In a DSS-induced mouse model of ulcerative colitis (UC), compound I exhibited significant anti-inflammatory efficacy. This work provides a potent Grp94 selective inhibitor as probe compound for the biol. study of Grp94 and represents the first study that confirms the potential therapeutic efficacy of Grp94-selective inhibitors against UC. In the experiment, the researchers used trans-4-Aminocyclohexanol(cas: 27489-62-9Product Details of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Product Details of 27489-62-9
Referemce:
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