3.2.1.10 (-)-1-azafagomine i.e.(3R,4R,5R)-4,5-dihydroxy-3-hydroxymethylhexahydropyridazine, competitive, slow inhibition process, difference in Ki values depend almost entirely on changes in the binding rate constant, direct binding model, some analogues of the compound are also inhibitory with less efficiency 55954 3.2.1.10 (2R,3S,4S)-1-[(2S,3S)-2,4-dihydroxy-3-(tridecyloxy)butyl]-3,4-dihydroxy-2-(hydroxymethyl)tetrahydrothiophenium - 28501 3.2.1.10 (2R,3S,4S)-1-[(2S,3S)-2,4-dihydroxy-3-methoxybutyl]-3,4-dihydroxy-2-(hydroxymethyl)tetrahydrothiophenium - 28499 3.2.1.10 (2R,3S,4S)-1-[(2S,3S)-3-(benzyloxy)-2,4-dihydroxybutyl]-3,4-dihydroxy-2-(hydroxymethyl)tetrahydrothiophenium - 28502 3.2.1.10 (2R,3S,4S)-1-[(2S,3S)-3-ethoxy-2,4-dihydroxybutyl]-3,4-dihydroxy-2-(hydroxymethyl)tetrahydrothiophenium - 28500 3.2.1.10 (2S,3S,4S,5S)-2-(hydroxymethyl)-5-[3-(4-methylphenyl)propyl]pyrrolidine-3,4-diol - 196657 3.2.1.10 (2S,3S,4S,5S)-2-(hydroxymethyl)-5-[4-(4-methoxyphenyl)butyl]pyrrolidine-3,4-diol - 196658 3.2.1.10 (2S,3S,4S,5S)-2-[4-(3,5-difluorophenyl)butyl]-5-(hydroxymethyl)pyrrolidine-3,4-diol good inhibition activities against intestinal isomaltase and sucrase 196659 3.2.1.10 1,2,3-tri-O-galloyl-beta-D-glucose about 20% inhibition at 1 mM 123073 3.2.1.10 1,4-anhydro-4-thio-D-arabinitol - 71578 3.2.1.10 1,4-dideoxy-1,4-((S)-[(2S,3S)-2,4-dihydroxy-3-butyl]episulfoniumylidene)-D-arabinitol - 72191 3.2.1.10 1,4-dideoxy-1,4-(hydroxyethyliminiumyl)-D-arabinitol - 71577 3.2.1.10 1,4-dideoxy-1,4-imino-D-arabinitol - 11086 3.2.1.10 1,4-dideoxy-1,4-imino-L-arabinitol - 38303 3.2.1.10 1,4-dideoxy-1,4-[(S)-[(2S,3S)-2,4-dihydroxy-3-(sulfooxy)butyl]episulfoniumylidene]-D-arabinitol - 147246 3.2.1.10 1,4-dideoxy-1,4-[(S)-[(2S,3S)-2,4-dihydroxy-3-butyl]episulfoniumylidene]-D-arabinitol - 147247 3.2.1.10 1,4-imino-1,2,4-trideoxy-D-arabinitol - 71576 3.2.1.10 1-O-Galloyl-beta-D-glucose about 15% inhibition at 1 mM, 34.4% inhibition at 5 mM 5457 3.2.1.10 1-O-methyl-2,3-di-O-galloyl-beta-D-glucose about 10% inhibition at 1 mM 123072 3.2.1.10 1-O-methyl-alpha-D-glucose 42% inhibition by 62 mM 90565 3.2.1.10 1-O-methyl-beta-D-glucose 52% inhibition by 62 mM 48426 3.2.1.10 2,5-dideoxy-2,5-imino-D-glucitol - 16479 3.2.1.10 2,5-dideoxy-2,5-imino-D-mannitol - 31734 3.2.1.10 2,5-dideoxy-2,5-imino-L-mannitol - 71575 3.2.1.10 2-Amino-2-ethyl-1,3-propanediol 80% inhibition of isomaltase activity by 50 mM 1742 3.2.1.10 2-amino-2-methyl-1,3-propanediol almost complete inhibition of isomaltase activity by 50 mM 9006 3.2.1.10 3'-O-methylponkoranol inhibits the different subunits to different extents, with extraordinary selectivity for C-terminal subunit of the enzyme 12176 3.2.1.10 4-nitrophenyl alpha-D-glucopyranoside - 1313 3.2.1.10 acarbose - 412 3.2.1.10 Ba2+ - 111 3.2.1.10 Ba2+ 72% inhibition by 2 mM BaCl2 111 3.2.1.10 blintol selenium analogue of salacinol 5404 3.2.1.10 Ca2+ 29% inhibition by 2 mM CaCl2 15 3.2.1.10 casuarictin ellagtannin, from flower buds of Syzygium aromaticum, about 16% inhibition at 1 mM 123070 3.2.1.10 Cd2+ complete inhibition 52 3.2.1.10 chymotrypsin almost 25% of palatinase activity after incubation with 0.1 mg/ml for 30 min 2434 3.2.1.10 Co2+ - 23 3.2.1.10 Co2+ complete inhibition 23 3.2.1.10 Co2+ 96% inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 23 3.2.1.10 conduritol-B-epoxide complete inactivation by 0.024 mM 8072 3.2.1.10 conduritol-B-epoxide - 8072 3.2.1.10 Cu2+ - 19 3.2.1.10 Cu2+ 96% inhibition by 2 mM CuCl2 19 3.2.1.10 Cu2+ 95% inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 19 3.2.1.10 Cu2+ complete inhibition by 1 mM CuCl2 19 3.2.1.10 D-glucose product inhibition, inhibition of 70.1% of activity by 110 mM 35 3.2.1.10 D-glucose - 35 3.2.1.10 D-glucose 52% inhibition by 10 mM, competitive 35 3.2.1.10 D-glucose sucrase-isomaltase gene expression is negatively regulated by glucose 35 3.2.1.10 D-glucose 22% inhibition at 0.7 mM, glucose product inhibition regulates the activities of both enzyme SI subunits 35 3.2.1.10 de-O-sulfonated kotalanol isolated from Salacia reticulata 6390 3.2.1.10 de-O-sulfonated kotalanol - 6390 3.2.1.10 de-O-sulfonated ponkoranol - 15214 3.2.1.10 de-O-sulfonated salacinol - 28540 3.2.1.10 diethanolamine about 80% inhibition of isomaltase activity by 50 mM 4809 3.2.1.10 DnaJ the coexpression of the Hsp70 team chaperone protein leads to reduced activity 9533 3.2.1.10 DnaK the coexpression of the Hsp70 team chaperone protein leads to reduced activity 123069 3.2.1.10 EDTA rapid loss of activity at 1 mM, pH 5.6, 76°C 21 3.2.1.10 EDTA no inhibition by 2 mM at pH 7.5 21 3.2.1.10 EDTA - 21 3.2.1.10 Elastase almost 50% of palatinase activity after incubation with 0.1 mg/ml for 30 min 12916 3.2.1.10 eugeniin ellagtannin, from flower buds of Syzygium aromaticum, about 18% inhibition at 1 mM 123071 3.2.1.10 Fe2+ complete inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 25 3.2.1.10 Fe2+ 90% inhibition by 1 mM FeCl2 25 3.2.1.10 Fe3+ 86% inhibition by 2 mM FeCl3 70 3.2.1.10 gallic acid 8% inhibition at 5mM 764 3.2.1.10 glucono-delta-lactone - 3470 3.2.1.10 glucono-delta-lactone 57% inhibition by 10 mM, competitive 3470 3.2.1.10 GrpE the coexpression of the Hsp70 team chaperone protein leads to reduced activity 13181 3.2.1.10 hepatocyte nuclear factor-1alpha gene expression of HNF-1alpha exhibits a positive correlation with that of sucrase-isomaltase regulated by glucose 141790 3.2.1.10 Hg2+ - 33 3.2.1.10 Hg2+ 99% inhibition by 2 mM HgCl2 33 3.2.1.10 Hg2+ complete inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 33 3.2.1.10 Hg2+ complete inhibition by 1 mM HgCl2 33 3.2.1.10 isofagomine stereoisomer of (-)-1-azafagomine, racemic, competitive 4362 3.2.1.10 isomaltose - 449 3.2.1.10 KCl 40% inhibition by 1 M 79 3.2.1.10 kotalanol - 3757 3.2.1.10 kotalanol isolated from Salacia reticulata 3757 3.2.1.10 maltose competitive inhibitor 86 3.2.1.10 maltose competitive; competitive; mixed 86 3.2.1.10 methyl alpha-D-glucopyranoside - 7494 3.2.1.10 Mg2+ 42% inhibition by 2 mM MgCl2 6 3.2.1.10 miglitol - 3392 3.2.1.10 Mn2+ 92% inhibition by 2 mM MbCl2 11 3.2.1.10 Mn2+ 40% inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 11 3.2.1.10 Monoethanolamine about 70% inhibition of isomaltase activity by 50 mM 20384 3.2.1.10 monoiodoacetate 77% inhibition by 1 mM 1473 3.2.1.10 additional information structure-activity relationship study of inhibitors, inhibitory effect of the inhibitors on the different enzyme activities, such as maltase, sucrase and isomaltase activity, overview, an increasing number of galloyl units in the molecule leads to an increase in inhibitory potency 2 3.2.1.10 additional information inhibition profiles of the individual N- and C-terminal catalytic subunits of the enzyme by clinical glucosidase inhibitors, acarbose and miglitol, and glucosidase inhibitors from an Ayurvedic remedy used for the treatment of type II diabetes, overview 2 3.2.1.10 mutant hepatocyte nuclear factor-1alpha in the wild HNF-1alpha cells SI gene expression and enzyme activity is not significantly diminished 141791 3.2.1.10 mutant hepatocyte nuclear factor-1beta in the wild HNF-1beta cells SI gene expression and enzyme activity is not significantly diminished 141792 3.2.1.10 N-ethylmaleimide 70% inactivation by 3.3 mM at room temperature after 10 min 49 3.2.1.10 NaCl 50% inhibition by 500 mM 42 3.2.1.10 Ni2+ 94% inhibition by 2 mM NiCl2 38 3.2.1.10 p-chloromercuribenzoate no inhibition by 2 mM with p-nitrophenyl-alpha-D-glucopyranoside as substrate 43 3.2.1.10 p-chloromercuribenzoate complete inhibition by 0.1 mM 43 3.2.1.10 p-nitrophenol - 151 3.2.1.10 p-nitrophenol complete inhibition by 2 mM 151 3.2.1.10 palatinose - 4277 3.2.1.10 papain proteolytic inactivation at 35°C, pH 6.8 3117 3.2.1.10 Pb2+ - 139 3.2.1.10 Pb2+ complete inhibition 139 3.2.1.10 Pb2+ 90% inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 139 3.2.1.10 Pb2+ complete inhibition by 1 mM PbCl2 139 3.2.1.10 penta-O-galloyl-beta-D-glucose about 40% inhibition at 1-5 mM 17611 3.2.1.10 phenol in combination with Tris most potent inhibitor 249 3.2.1.10 phenyl alpha-D-glucoside - 6012 3.2.1.10 phenyl alpha-D-glucoside 58% inhibition by 10 mM 6012 3.2.1.10 Phenyl alpha-maltoside 92% inhibition by 10 mM, noncompetitive 3104 3.2.1.10 pronase E proteolytic inactivation at 35°C, pH 6.8 31909 3.2.1.10 salacinol isolated from Salacia reticulata 2616 3.2.1.10 salacinol - 2616 3.2.1.10 SDS 96% inhibition by 3.5 mM under standard conditions 124 3.2.1.10 Sn2+ complete inhibition 413 3.2.1.10 subtilisin BPN' proteolytic inactivation at 35°C, pH 6.8 31155 3.2.1.10 sucrose - 55 3.2.1.10 triethanolamine about 80% inhibition of isomaltase activity by 50 mM 3368 3.2.1.10 Tris complete inhibition of isomaltase activity by 50 mM 317 3.2.1.10 Tris - 317 3.2.1.10 Tris 89% inhibition by 5 mM, competitive 317 3.2.1.10 Tris 93% inhibition by 5 mM 317 3.2.1.10 Trypsin almost 25% of palatinase activity after incubation with 0.1 mg/ml for 30 min 393 3.2.1.10 Trypsin proteolytic inactivation at 35°C, pH 6.8 393 3.2.1.10 Urea 26% inhibition by 4 mM under standard conditions 116 3.2.1.10 Urea - 116 3.2.1.10 Urea 50% inactivation after treatment with 8.7 M for 5 h at 25°C or 2.4 M at 60°C and pH 6.8 116 3.2.1.10 Urea 50% inactivation after treatment with 9.2 M for 5 h at 25°C or 2.7 M at 60°C and pH 6.8 116 3.2.1.10 Urea 50% inactivation after treatment with 4.6 M for 5 h at 25°C and pH 6.8 116 3.2.1.10 Urea 50% inactivation after treatment with 1.42 M at 25°C or 0.74 M at 35°C for 5 h 116 3.2.1.10 Zn2+ rapid inactivation by 1 mM possibly through interaction with free thiol groups of the enzyme 14 3.2.1.10 Zn2+ - 14 3.2.1.10 Zn2+ complete inhibition 14 3.2.1.10 Zn2+ 96% inhibition by 2 mM in 20 mM borate buffer, pH 7.5 with p-nitrophenyl-alpha-D-glucopyranoside as substrate 14 3.2.1.10 Zn2+ 99% inhibition by 1 mM ZnCl2 14