3.2.1.24 (1R,6R,7R,8S)-7,8-dihydroxy-5-thia-1-thioniabicyclo[4.3.0]nonane chloride synthetic inhibitor, selective and potent inhibition at 1 mM, 97% inhibition of the activity of the liver lysosomal fraction at pH 4.0, 100% at pH 6.5 58316 3.2.1.24 (1S,2R,3R,8R,8aR)-3-[(arylmethoxy)methyl]octahydroindolizine-1,2,8-triol - 129335 3.2.1.24 (1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol - 10175 3.2.1.24 (2R,3R,4S)-2-(aminomethyl)pyrrolidine-3,4-diol 1 mM, 81% inhibition, competitive 33672 3.2.1.24 (2R,3R,4S)-2-(aminomethyl)pyrrolidine-3,4-diol 1 mM, 51% inhibition 33672 3.2.1.24 (2R,3R,4S)-2-([(1R)-2,3-dihydro-1H-inden-1-ylamino]methyl)pyrrolidine-3,4-diol IC50 is 0.017 mM 35381 3.2.1.24 (2R,3R,4S)-2-([[(1R)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol 1 mM, 75% inhibition, competitive 33673 3.2.1.24 (2R,3R,4S)-2-([[(1R)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol 1 mM, 39% inhibition 33673 3.2.1.24 (2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol - 6284 3.2.1.24 (2R,3R,4S)-2-([[(1S)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol 1 mM, 66% inhibition, competitive 33674 3.2.1.24 (2R,3R,4S)-2-([[(1S)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol 1 mM, 45% inhibition 33674 3.2.1.24 (2R,3R,4S)-2-hydroxymethyl-pyrrolidine-3,4-diol 1 mM, 54% inhibition 53591 3.2.1.24 (2R,3R,4S)-2-hydroxymethyl-pyrrolidine-3,4-diol 1 mM, 37% inhibition 53591 3.2.1.24 (2R,3R,4S)-2-phenylaminomethyl-pyrrolidine-3,4-diol 1 mM, 92% inhibition, competitive 22464 3.2.1.24 (2R,3R,4S)-2-phenylaminomethyl-pyrrolidine-3,4-diol 1 mM, 69% inhibition, competitive 22464 3.2.1.24 (2R,3R,4S)-2-[(1-phenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol 1 mM, 66% inhibition, competitive 33675 3.2.1.24 (2R,3R,4S)-2-[(1-phenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol 1 mM, 48% inhibition 33675 3.2.1.24 (2R,3R,4S)-2-[(benzylamino)methyl]pyrrolidine-3,4-diol IC50 is 0.06 mM 35380 3.2.1.24 (2R,3R,4S)-2-[(cyclopentylamino)methyl]pyrrolidine-3,4-diol 1 mM, 60% inhibition 53588 3.2.1.24 (2R,3R,4S)-2-[(cyclopentylamino)methyl]pyrrolidine-3,4-diol 1 mM, 53% inhibition 53588 3.2.1.24 (2R,3R,4S)-2-[([(1R)-2-benzyloxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol 92% inhibition at 1 mM, IC50 is 0.058 mM 35459 3.2.1.24 (2R,3R,4S)-2-[([(1R)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol complete and selective inhibition at 1 mM, IC50 is 700 nM 17893 3.2.1.24 (2R,3R,4S)-2-[([(1R)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol potent and selective inhibition 17893 3.2.1.24 (2R,3R,4S)-2-[([(1R)-2-methoxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol 77% inhibition at 1 mM 129739 3.2.1.24 (2R,3R,4S)-2-[([(1R,2S)-2-hydroxy-1,2-diphenylethyl]amino)methyl]pyrrolidine-3,4-diol 88% inhibition at 1 mM, IC50 is 0.11 mM 58953 3.2.1.24 (2R,3R,4S)-2-[([(1S)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol 92% inhibition at 1 mM, IC50 is 0.1 mM 35456 3.2.1.24 (2R,3R,4S)-2-[([(1S)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol - 35456 3.2.1.24 (2R,3R,4S)-2-[([(1S,2R)-2-hydroxy-1,2-diphenylethyl]amino)methyl]pyrrolidine-3,4-diol 84% inhibition at 1 mM, IC50 is 0.128 mM 58954 3.2.1.24 (2R,3R,4S)-2-[2-(phenylamino)ethyl]pyrrolidine-3,4-diol 1 mM, 33% inhibition 117414 3.2.1.24 (2R,3R,4S)-2-[[(1-benzyl-piperidin-4-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 55% inhibition 53589 3.2.1.24 (2R,3R,4S)-2-[[(1-benzyl-piperidin-4-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 59% inhibition 53589 3.2.1.24 (2R,3R,4S)-2-[[(2H-Imidazol-1-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 55% inhibition 33676 3.2.1.24 (2R,3R,4S)-2-[[(2H-Imidazol-1-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 59% inhibition 33676 3.2.1.24 (2R,3R,4S)-2-[[(furan-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 49% inhibition 53590 3.2.1.24 (2R,3R,4S)-2-[[(furan-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 29% inhibition 53590 3.2.1.24 (2R,3R,4S)-2-[[(thiophen-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 89% inhibition, competitive 22463 3.2.1.24 (2R,3R,4S)-2-[[(thiophen-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol 1 mM, 68% inhibition, competitive 22463 3.2.1.24 (2R,3R,4S,5R)-2-[(benzylamino)methyl]-5-(hydroxymethyl)pyrrolidine-3,4-diol IC50 is 0.0062 mM 35382 3.2.1.24 (2R,3S,4R,5R)-2-(hydroxymethyl)-5-[([(1R)-2-hydroxy-1,2-diphenylethyl]amino)methyl]pyrrolidine-3,4-diol 98% inhibition at 1 mM, IC50 is 0.0042 mM 35458 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 2-fluorobenzoate 83% inhibition at 1 mM, IC50 is 0.063 mM 23749 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 2-fluorobenzoate - 23749 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 3-bromobenzoate 79% inhibition at 1 mM 58951 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 3-bromobenzoate - 58951 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-bromobenzoate 92% inhibition at 1 mM 58952 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-bromobenzoate - 58952 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-fluorobenzoate 92% inhibition at 1 mM, IC50 is 0.060 mM 23750 3.2.1.24 (2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-fluorobenzoate - 23750 3.2.1.24 (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one - 7769 3.2.1.24 (3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one - 7770 3.2.1.24 (3S,4R)-pyrrolidine-3,4-diol 1 mM, 70% inhibition 53592 3.2.1.24 (3S,4R)-pyrrolidine-3,4-diol 1 mM, 40% inhibition 53592 3.2.1.24 (6-butoxy-3-oxo-3,6-dihydro-2H-pyran-2-yl)methyl 2,2-dimethylpropanoate - 197496 3.2.1.24 (6-methoxy-3-oxo-3,6-dihydro-2H-pyran-2-yl)methyl 2,2-dimethylpropanoate - 197495 3.2.1.24 1,4-Dideoxy-1,4-imino-D-mannitol - 5452 3.2.1.24 1,6-dideoxy-1,6-episulfinyl-beta-D-mannose XLM, sulfoxide derivative, thiolevomannosan analog, more potent than kifunensine and deoxymannojirimycin, docking studies with the crystal structure of human alpha-1,2-mannosidase complexed with kifunensine (PDB: 1FO3) as a template 66233 3.2.1.24 1,6-dideoxy-1,6-episulfonyl-beta-D-mannose NLM, sulfone derivative, thiolevomannosan analog, more potent than kifunensine and deoxymannojirimycin, docking studies with the crystal structure of human alpha-1,2-mannosidase complexed with kifunensine (PDB: 1FO3) as a template 66234 3.2.1.24 1,6-dideoxy-1,6-epithio-beta-D-mannose thiolevomannosan TLM, docking studies with the crystal structure of human alpha-1,2-mannosidase complexed with kifunensine (PDB: 1FO3) as a template 66232 3.2.1.24 1-cyclohexyl-3-(2-morpholinyl-4-ethyl)carbodiimide inhibitory at 25 mM, pseudo-first-order kinetic 102030 3.2.1.24 1-deoxy-mannojirimycin complete inhibition 151333 3.2.1.24 1-deoxymannojirimicin hydrolysis of 4-methylumbelliferyl-alpha-D-mannnopyranoside, strong inhibition for enzymes I and II at 0.025 mM 11048 3.2.1.24 1-deoxymannojirimicin complete inhibition at 1 mM 11048 3.2.1.24 1-deoxymannojirimicin 19% inhibition at 0.01 mM 11048 3.2.1.24 1-deoxymannojirimicin IC50 = 0.01 mM 11048 3.2.1.24 1-deoxymannojirimicin 67% inhibition at 1 mM when 4-methylumbelliferyl-alpha-D-mannopyranoside is used, 15% inhibition when p-nitrophenyl-alpha-D-mannopyranoside is used as substrates 11048 3.2.1.24 1-deoxymannojirimicin 50% inhibition at 0.05 mM 11048 3.2.1.24 1-deoxymannojirimycin mannose analog, in vivo and in vitro; reversible (not by Ca2+) 1183 3.2.1.24 1-deoxymannojirimycin - 1183 3.2.1.24 1-deoxymannojirimycin 61% inhibition of the activity of the liver lysosomal fraction at pH 4.0, 37% at pH 6.5, at 1 mM 1183 3.2.1.24 1-deoxymannojirimycin class 1 alpha1,2-mannosidase inhibitor 1183 3.2.1.24 1-deoxymannojirimycin binding of swainsonine to the enzyme is stronger than bionding of 1-deoxymannojirimycin; competitive inhibitor, low binding up to 40°C, increased binding at 50°C 1183 3.2.1.24 1-deoxymannojirimycin pretreatment with 1-deoxymannojirimycin protectes primary cultured mouse cortical neurons from Amyloid beta1-42 toxicity 1183 3.2.1.24 1-deoxymannojirimycin pretreatment with 100 mM inhibitor 1-deoxymannojirimycin in PC-12 cells significantly attenuates the cytotoxicity by endoplasmic reticulum stressors tunicamycin, thapsigargin, and amyloid bbeta1-42, and reduces caspase-3 activation by tunicamycin and thapsigarin 1183 3.2.1.24 2-(2,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol 1 mM, 81% inhibition, mixed type 33671 3.2.1.24 2-(2,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol 1 mM, 56% inhibition 33671 3.2.1.24 2-amino-2-deoxy-D-glucose competitive inhibition, Ki = 2.8 mM 6101 3.2.1.24 2-deoxy-2-fluoro-alpha-D-mannosyl fluoride for mutant enzyme D341N, no inhibition of wild-type enzyme 11277 3.2.1.24 3-bromo-N-[(2S)-2-[([(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl]benzamide 95% inhibition at 1 mM, IC50 is 0.089 mM 35457 3.2.1.24 3-bromo-N-[(2S)-2-[([(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl]benzamide - 35457 3.2.1.24 5-fluoro-beta-L-gulosyl fluoride reversible, acts as a slow substrate for the D341 mutant enzyme, with deglycosylation as the rate-limiting step. Inactivation is only observed when assayed at low temperatures such that deglycosylation is slow relative to the assay time 8491 3.2.1.24 8,8a-di-epi-swainsonine - 23745 3.2.1.24 8a-epi-swainsonine - 23746 3.2.1.24 Ag+ slight inhibition at 1 mM for isoforms I, II 75 3.2.1.24 Ag+ moderate inhibition at 1 mM 75 3.2.1.24 Ag+ 70% inhibition at 1 mM 75 3.2.1.24 Ag+ 97% inhibition at 10 mM 75 3.2.1.24 Ag+ 52% inhibition at 10 mM 75 3.2.1.24 Ag+ - 75 3.2.1.24 Ag+ strong inhibitor at concentrations of 1 mM or 10 mM 75 3.2.1.24 alpha-conglutin 11% inhibition at saturation 47797 3.2.1.24 alpha-D-1,2-mannopyranosyl-mannopyranose 50% inhibition at 4 mM 108663 3.2.1.24 alpha-D-1,3-mannopyranosyl-alpha-D-mannopyranose 50% inhibition at 18 mM 108664 3.2.1.24 alpha-D-1,6-mannopyranosyl-mannopyranose 50% inhibition at 100 mM 108665 3.2.1.24 alpha-D-mannopyranose 55% inhibition at 30 mM 756 3.2.1.24 alpha-D-mannopyranose 27% inhibition at 10 mM 756 3.2.1.24 alpha-D-mannopyranose competitive inhibition, Ki: 22 mM 756 3.2.1.24 alpha-D-mannopyranose 50% inhibition at 250 mM 756 3.2.1.24 alpha-D-mannopyranose 29% inhibition at 10 mM 756 3.2.1.24 alpha-D-mannopyranose competitive inhibition, Ki: 85 mM 756 3.2.1.24 alpha-D-mannopyranose competitive inhibition, Ki: 20 mM 756 3.2.1.24 alpha-D-mannopyranose 30% inhibition at 250 mM 756 3.2.1.24 Ba2+ 10 mM; 78% inhibition at 10 mM 111 3.2.1.24 Ba2+ inhibition at 1 mM 111 3.2.1.24 Ca2+ inhibitory for enzyme I above 5 mM, enzyme II not affected 15 3.2.1.24 Ca2+ 53% inhibition at 0.1 mM 15 3.2.1.24 Ca2+ slight inhibition at 1 mM 15 3.2.1.24 Ca2+ inhibition at 0.1 mM 15 3.2.1.24 Cd2+ 10 mM, activation at 1 mM; 54% inhibition at 10 mM, slight stimulation at 1 mM 52 3.2.1.24 Cd2+ - 52 3.2.1.24 Cd2+ inhibition at 0.1 mM 52 3.2.1.24 Co2+ 46% inhibition at 1 mM 23 3.2.1.24 Co2+ slight inhibition at 1 mM 23 3.2.1.24 Co2+ 57% inhibition at 1 mM 23 3.2.1.24 Co2+ slight inhibition at 10 mM 23 3.2.1.24 Co2+ inhibition of alpha-mannosidases IA and IB 23 3.2.1.24 Co2+ 51% inhibition at 10 mM 23 3.2.1.24 Co2+ 10-30% inhibition for acid alpha-mannosidase 23 3.2.1.24 Co2+ - 23 3.2.1.24 Cu2+ complete inhibition of the Co2+ activated enzyme at 0.5 mM 19 3.2.1.24 Cu2+ complete inhibition at 1 mM 19 3.2.1.24 Cu2+ complete inhibition at 0.1 mM 19 3.2.1.24 Cu2+ strong inhibition at 1 mM 19 3.2.1.24 Cu2+ nearly complete inhibition at 0.01 mM 19 3.2.1.24 Cu2+ slight inhibition at 0.1 mM 19 3.2.1.24 Cu2+ slight inhibition at 10 mM 19 3.2.1.24 Cu2+ - 19 3.2.1.24 Cu2+ inhibition of alpha-mannosidases IA, IB and II 19 3.2.1.24 Cu2+ 10% inhibition at 10 mM, alpha-mannosidase A 19 3.2.1.24 Cu2+ 10 mM; 41% inhibition at 10 mM 19 3.2.1.24 Cu2+ 87% inhibition at 20 mM 19 3.2.1.24 Cu2+ potent inhibitor 19 3.2.1.24 Cu2+ nearly complete inhibition at 0.005 mM 19 3.2.1.24 Cu2+ inhibition at 0.1 mM 19 3.2.1.24 Cu2+ strong inhibitor at concentrations of 1 mM or 10 mM 19 3.2.1.24 Cu2+ inhibits in presence of Co2+ 19 3.2.1.24 cysteine 31% inhibition at 0.02 mM 153 3.2.1.24 D-glucose 67% inhibition at 30 mM 35 3.2.1.24 D-glucuronic acid slight inhibition at 10 mM 1498 3.2.1.24 D-mannono-1,4-lactone 11% inhibition at 10 mM 11057 3.2.1.24 D-mannono-1,4-lactone 36% inhibition at 10 mM 11057 3.2.1.24 D-mannono-1,4-lactone Ki: 23.8 mM 11057 3.2.1.24 D-mannono-1,4-lactone competitive inhibition, Ki: 13 mM 11057 3.2.1.24 D-mannono-1,5-lactone 50% competitive inhibition at 0.073 mM 5537 3.2.1.24 D-mannono-1,5-lactone complete inhibition at 1 mM 5537 3.2.1.24 D-mannono-1,5-lactone weak inhibition 5537 3.2.1.24 D-mannono-gamma-lactone - 43997 3.2.1.24 D-mannosylamine 56% inhibition at 1 mM 21294 3.2.1.24 D-mannosylamine 15% competitive inhibition at 5 mM 21294 3.2.1.24 D-mannosylamine - 21294 3.2.1.24 D-mannosylamine competitive inhibition, Ki = 0.007 mM 21294 3.2.1.24 deoxymannojirimycin - 6174 3.2.1.24 deoxymannojirimycin less effective compared with swainsonine, concentration of 100 microM 6174 3.2.1.24 deoxymannojirimycin DMJ 3 6174 3.2.1.24 diisopropylfluorophosphate 42% inhibition at 10 mM 299 3.2.1.24 EDTA complete inhibition at 20 mM, activity recovered in the presence of Ca2+ 21 3.2.1.24 EDTA complete inhibition at 0.05 mM 21 3.2.1.24 EDTA 37% inhibition at 5 mM 21 3.2.1.24 EDTA strong inhibition at 1 mM 21 3.2.1.24 EDTA complete inhibition at 1 mM, addition of 1 mM Zn2+ fully restores activity for isoforms II, to 69% for isoforms I 21 3.2.1.24 EDTA addition of Zn2+ restores inhibitory effect 21 3.2.1.24 EDTA slight inhibition at 1 mM 21 3.2.1.24 EDTA 60-75% inhibition at 4 mM, activity restored by addition of Ca2+ 21 3.2.1.24 EDTA inhibitory for alpha-mannosidases IA and IB 21 3.2.1.24 EDTA addition of Zn2+ restores inhibitory effect; strong inhibition at 1 mM 21 3.2.1.24 EDTA complete inactivition, Zn2+ restores, Ca2+, Cd2+, Mg2+, Ni2+, Na+ or Cu2+ restore partly 21 3.2.1.24 EDTA 1 mM, more than 90% inactivation 21 3.2.1.24 EDTA - 21 3.2.1.24 EDTA supplied in equimolar amounts or in excess, neutralizes also effect of resistance of ManA to heat inactivation 21 3.2.1.24 EGTA 32% inhibition at 5 mM 173 3.2.1.24 Fe2+ 54% inhibition at 1 mM 25 3.2.1.24 Fe2+ slight inhibition at 1 mM 25 3.2.1.24 Fe2+ complete inhibition at 1 mM 25 3.2.1.24 Fe2+ nearly complete inhibition at 1 mM 25 3.2.1.24 Fe2+ slight inhibition at 10 mM 25 3.2.1.24 Fe2+ - 25 3.2.1.24 Fe2+ 58% inhibition at 10 mM 25 3.2.1.24 Fe2+ 22% inhibition at 20 mM 25 3.2.1.24 Fe2+ potent inhibitor 25 3.2.1.24 Fe3+ 43% inhibition at 1 mM 70 3.2.1.24 Fe3+ - 70 3.2.1.24 Fe3+ inhibition at 1 mM 70 3.2.1.24 Fe3+ strong inhibitor at concentrations of 1 mM or 10 mM 70 3.2.1.24 gluco-hydroxyiminolactam - 18894 3.2.1.24 glucoimidazole - 11962 3.2.1.24 Hg2+ complete inhibition at 1 mM 33 3.2.1.24 Hg2+ slight inhibition at 1 mM for isoforms I,II 33 3.2.1.24 Hg2+ - 33 3.2.1.24 Hg2+ 45% inhibition at 10 mM 33 3.2.1.24 Hg2+ complete inhibition at 10 mM 33 3.2.1.24 Hg2+ strong inhibitor 33 3.2.1.24 iodoacetamide slight inhibition at 1 mM 67 3.2.1.24 iodoacetic acid slight inhibition at 1 mM 213 3.2.1.24 iodoacetic acid - 213 3.2.1.24 iodoacetic acid slight inhibition at 0.1 mM 213 3.2.1.24 kifunensine class 1 alpha1,2-mannosidase inhibitor 1980 3.2.1.24 kifunensine little inhibitory effect, concentration of 10 microM 1980 3.2.1.24 kifunensine Kif 2, docking studies with the crystal structure of human alpha-1,2-mannosidase complexed with kifunensine (PDB: 1FO3) as a template 1980 3.2.1.24 kifunensine - 1980 3.2.1.24 Li+ 88% inhibition at 20 mM 152 3.2.1.24 Mannan 33% inhibition at 50 mM 5574 3.2.1.24 mannoimidazole - 14557 3.2.1.24 mannose relative inhibition of 67.8%, potent inhibitor, three concentrations of 10, 50, and 100 mM tested 988 3.2.1.24 methyl-alpha-D-glucoside 23% inhibition at 10 mM 3351 3.2.1.24 methyl-alpha-D-lyxopyranosyl-(1'-2)-alpha-D-mannopyranoside - 56394 3.2.1.24 methyl-alpha-D-lyxopyranosyl-(1-2)-alpha-D-mannopyranoside potent 123098 3.2.1.24 methyl-alpha-D-mannopyranoside 41% inhibition at 10 mM 9473 3.2.1.24 methyl-alpha-D-mannopyranoside 20% inhibition at 10 mM 9473 3.2.1.24 methyl-alpha-D-mannopyranoside slight inhibitory for alpha-mannosidases IA and IB 9473 3.2.1.24 methyl-alpha-D-mannopyranoside 37% inhibition at 0.1 mM 9473 3.2.1.24 methyl-alpha-D-mannopyranoside 40-50% inhibition of acid alpha-mannosidase, neutral alpha-mannosidase not affected 9473 3.2.1.24 methyl-alpha-mannoside not 20377 3.2.1.24 Mg2+ slight inhibition at 1 mM 6 3.2.1.24 Mg2+ - 6 3.2.1.24 Mg2+ 61% inhibition at 20 mM 6 3.2.1.24 Mg2+ inhibition at 1 mM 6 3.2.1.24 Mn2+ inhibitory for enzyme I above 5 mM, slightly inhibitory for enzyme II 11 3.2.1.24 Mn2+ slight inhibition at 1 mM 11 3.2.1.24 Mn2+ 58% inhibition at 0.1 mM 11 3.2.1.24 Mn2+ complete inhibition at 1 mM 11 3.2.1.24 Mn2+ - 11 3.2.1.24 Mn2+ inhibition at 1 mM 11 3.2.1.24 additional information no inhibition by L-cysteine 2 3.2.1.24 additional information no inhibition by Mg2+ 2 3.2.1.24 additional information no inhibition by 1-deoxymannojirimycin 2 3.2.1.24 additional information no inhibition by (2R,3R,4S)-2-[(2-hydroxy-1-methyl-2,2-diphenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol, and (2R,3R,4S)-2-(1,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol 2 3.2.1.24 additional information no inhibition by (2R,3R,4S)-2-[(2-hydroxy-1-methyl-2,2-diphenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol, (2R,3R,4S)-2-(1,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol, and (2R,3R,4S)-2-[2-(phenylamino)ethyl]pyrrolidine-3,4-diol 2 3.2.1.24 additional information inhibition of growth of glioblastoma and melanoma cells by pyrrolidine-3,4-diol derivatives, overview 2 3.2.1.24 additional information down-regulation of Man2C1 activity by a small interfering RNA drastically change amount and structure of oligosaccharides accumulating in the cytosol, demonstrating that Man2C1 is involved in free oligosaccharide processing in the cytosol 2 3.2.1.24 additional information inhibitory activity of thiosugar derivatives (thiolevomannosans) is tested against alpha-mannosidase 2 3.2.1.24 additional information 1-deoxymannojirimycin has no effect on ManA at concentrations up to 500 microM 2 3.2.1.24 additional information not inhibitory: 1,5-D-mannoseptanosyl di- and trisaccharide ring-size isomers 2 3.2.1.24 additional information activity is insensitive to 1-deoxymannojirimycin at concentration up to 2 mM. No change in the enzymatic activity is observed with 0.001-1 mM EDTA 2 3.2.1.24 N-bromosuccinimide N-bromosuccinimide modified inactivation, effect of Trp modification on enzyme activity 208 3.2.1.24 N-octyl-6-epi-valienamine - 18896 3.2.1.24 Na+ 1 mM, weak, not at 10 mM 59 3.2.1.24 NaN3 slight inhibition at 0.1 mM 238 3.2.1.24 Ni2+ moderate inhibition at 1 mM 38 3.2.1.24 Ni2+ strong inhibitor at concentrations of 1 mM or 10 mM 38 3.2.1.24 Ni2+ inhibits in presence of Co2+ 38 3.2.1.24 noeuromycin - 11797 3.2.1.24 p-chloromercuribenzenesulfonic acid strong inhibition at 1 mM 3485 3.2.1.24 p-chloromercuribenzenesulfonic acid complete inhibition at 1 mM 3485 3.2.1.24 p-chloromercuribenzenesulfonic acid different inhibition rates for alpha-mannosidases IA, IB and II 3485 3.2.1.24 p-chloromercuribenzenesulfonic acid 50% inhibition at 0.35 mM, activity is restored by addition of substrate 3485 3.2.1.24 p-nitrophenyl-alpha-D-mannopyranoside substrate inhibition greater than 2 mM 1562 3.2.1.24 Pb2+ complete inhibition of the Co2+ activated enzyme at 0.5 mM 139 3.2.1.24 Pb2+ moderate inhibition at 1 mM 139 3.2.1.24 SDS 85% inhibition at 0.05%, w/v 124 3.2.1.24 small interfering RNA siRNA designed to specifically inhibit Man2C1 gene expression, alpha-mannosidase activity is compromised in siRNA-treated cells. Determination of alteration of siRNA treatment, glycans recovered from membrane glycoproteins are fluorescence-labelled and analysed by HPLC 54448 3.2.1.24 Sr2+ inhibition at 1 mM 338 3.2.1.24 swainsonine hydrolysis of 4-umbelliferyl-alpha-D-mannopyranoside, strong inhibition for enzymes I and II at 0.025 mM 646 3.2.1.24 swainsonine 50% inhibition at 0.00024 mM 646 3.2.1.24 swainsonine IC50: 0.00015 mM 646 3.2.1.24 swainsonine complete inhibition of the Co2+ activated enzyme at 0.01 mM 646 3.2.1.24 swainsonine IC50: 0.00011 mM 646 3.2.1.24 swainsonine inhibition of both Tris-eluted and unbound isoforms from cobalt-chelating Sepharose, unbound: Ki: 0.028 mM, Tris-eluted: Ki: 0.004 mM 646 3.2.1.24 swainsonine 83% inhibition at 0.3 mM if 4-methylumbelliferyl-alpha-D-mannopyranoside is used, hydrolysis of p-nitrophenyl-alpha-D-mannopyranoside only slightly diminished at 0.3 mM 646 3.2.1.24 swainsonine complete inhibition at 0.008 mM 646 3.2.1.24 swainsonine 50% inhibition in the range of 0.3-0.6 mM 646 3.2.1.24 swainsonine competitive inhibition 646 3.2.1.24 swainsonine competitive inhibition, Ki: 0.00036 mM 646 3.2.1.24 swainsonine complete inhibition 646 3.2.1.24 swainsonine IC50: 10 nM 646 3.2.1.24 swainsonine competitive 646 3.2.1.24 swainsonine - 646 3.2.1.24 swainsonine potent inhibition at 1 mM, 100% inhibition of the activity of the liver lysosomal fraction at pH 4.0, 95% at pH 6.5 646 3.2.1.24 swainsonine IC50 is 400 nM 646 3.2.1.24 swainsonine 20% inhibition of glioblastoma cell growth at 0.25 mM 646 3.2.1.24 swainsonine concentration of 100 microM 646 3.2.1.24 swainsonine shows competitive inhibition when p-nitrophenyl-Man is used as a substrate 646 3.2.1.24 swainsonine binding of swainsonine to the enzyme is stronger than bionding of 1-deoxymannojirimycin; competitive inhibitor, low binding up to 40°C, increased binding at 50°C 646 3.2.1.24 swainsonine binding structure, overview 646 3.2.1.24 swainsonine the enzyme substituted with Zn2+ is considerably less sensitive to swainsonine compared with the Co2+-, Cd2+-, and Mn2+-substituted enzyme 646 3.2.1.24 swainsonine swainsonine treatment completely inhibits the acid enzyme form activity below pH 5.0 646 3.2.1.24 Tris inhibitory for alpha-mannosidases IA and IB 317 3.2.1.24 Tris in vivo and in vitro 317 3.2.1.24 Zn2+ complete inhibition of the Co2+ activated enzyme at 0.5 mM 14 3.2.1.24 Zn2+ complete inhibition at 1 mM 14 3.2.1.24 Zn2+ strong inhibition at 1 mM 14 3.2.1.24 Zn2+ moderate inhibition at 1 mM 14 3.2.1.24 Zn2+ slight inhibition for alpha-mannosidase IA 14 3.2.1.24 Zn2+ 55% inhibition at 10 mM 14 3.2.1.24 Zn2+ - 14 3.2.1.24 Zn2+ 25% inhibition at 20 mM 14 3.2.1.24 Zn2+ inhibition at 1 mM 14 3.2.1.24 Zn2+ reversible by Ca2+ 14 3.2.1.24 Zn2+ mutant enzymes H228Q, H533E, and H533Q, are all inhibited by high Zn2+ concentrations (1 mM) 14 3.2.1.24 ZnCl2 92% inhibition by 1 mM, 56% inhibition by 0.01 mM 271 3.2.1.24 [6-(3-methylbutoxy)-3-oxo-3,6-dihydro-2H-pyran-2-yl]acetonitrile - 197497 3.2.1.24 [6-(3-methylbutoxy)-3-oxo-3,6-dihydro-2H-pyran-2-yl]methyl 2,2-dimethylpropanoate - 197494 3.2.1.24 [[(3S,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)piperidin-2-ylidene]amino] N-(4-chlorophenyl)carbamate - 26163