Kifunensine

Kifunensine was originally isolated from the actinomycete Kitasatosporia kifunensine No. 9482 and shown to be a weak inhibitor of aryl mannosidase. It has since been shown to be a potent and selective inhibitor of class I alpha-mannosidases and may serve as a key inhibitor of glycoprotein biosynthesis. Kifunensine inhibits both human endoplasmic reticulum alpha-1,2-mannosidase I and members of the Golgi subfamily of the class I mannosidases (Golgi alpha-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM, respectively. It also inhibits mung bean alpha-1,2-mannosidase I with an IC50 value of 20-50 nM. Kifunensine can be used to block alpha-mannosidase I activity at the endoplasmic reticulum (ER), preventing the removal of desired mutated proteins through ER quality control mechanisms.Formal Name: hexahydro-6R,7S,8aS-trihydroxy-5R-(hydroxymethyl)-imidazo[1,2-a]pyridine-2,3-dione. CAS Number: 109944-15-2. Synonyms: FR900494. Molecular Formula: C8H12N2O6. Formula Weight: 232.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Warm Distilled Water: 0.5 mg/ml. lambdamax: 225 nm. SMILES: O[C@H]1[C@H](O)[C@H](O)[C@](NC(C2=O)=O)([H])N2[C@@H]1CO. InChi Code: InChI=1S/C8H12N2O6/c11-1-2-3(12)4(13)5(14)6-9-7(15)8(16)10(2)6/h2-6,11-14H,1H2,(H,9,15)/t2-,3-,4+,5+,6+/m1/s1. InChi Key: OIURYJWYVIAOCW-PQMKYFCFSA-N.