Perpropanoyl kifunensine | CAS 2762179-07-5

FC-141

Synonyms:  (5R,6R,7S,8R)-2,3-dioxo-5-((propionyloxy)methyl)octahydroimidazo[1,2-a]pyridine-6,7,8-triyl tripropionate

These ester derivatives (along with the perbutanoyl analogue) of kifunensine are the most potent mannosidase I inhibitors in cellular assays described to date. The propionate ester demonstrated a 50-fold higher potency compared to kifunensine due to their increased lipophilicity. This improved activity allows nM instead of µM concentrations to be used.^1,2

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¹ Kurhade, S. E.; Weiner, J. D.; Gao, F. P.; Farrell, M. P., Functionalized High Mannose-Specific Lectins for the Discovery of Type I Mannosidase Inhibitors. Angew. Chem. Int. Ed. 2021, 60 (22), 12313-12318.

² Huang, A.; Kurhade, S. E.; Ross, P.; Apley, K. D.; Griffin, J. D.; Berkland, C. J.; Farrell, M. P., Disrupting N-Glycosylation Using Type I Mannosidase Inhibitors Alters B-Cell Receptor Signaling. ACS Pharmacology & Translational Science 2022, 5 (11), 1062-1069. 

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