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(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
(1S,2R,3R,8R,8aR)-3-[(arylmethoxy)methyl]octahydroindolizine-1,2,8-triol
-
-
(1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
(2R,3R,4S)-2-(aminomethyl)pyrrolidine-3,4-diol
(2R,3R,4S)-2-([(1R)-2,3-dihydro-1H-inden-1-ylamino]methyl)pyrrolidine-3,4-diol
-
IC50 is 0.017 mM
(2R,3R,4S)-2-([[(1R)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
(2R,3R,4S)-2-([[(1S)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol
(2R,3R,4S)-2-hydroxymethyl-pyrrolidine-3,4-diol
(2R,3R,4S)-2-phenylaminomethyl-pyrrolidine-3,4-diol
(2R,3R,4S)-2-[(1-phenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol
(2R,3R,4S)-2-[(benzylamino)methyl]pyrrolidine-3,4-diol
-
IC50 is 0.06 mM
(2R,3R,4S)-2-[(cyclopentylamino)methyl]pyrrolidine-3,4-diol
(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
(2R,3R,4S)-2-[([(1R)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol
(2R,3R,4S)-2-[([(1R)-2-methoxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol
-
77% inhibition at 1 mM
(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
(2R,3R,4S)-2-[([(1S)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol
(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
(2R,3R,4S)-2-[2-(phenylamino)ethyl]pyrrolidine-3,4-diol
-
1 mM, 33% inhibition
(2R,3R,4S)-2-[[(1-benzyl-piperidin-4-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
(2R,3R,4S)-2-[[(2H-Imidazol-1-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
(2R,3R,4S)-2-[[(furan-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
(2R,3R,4S)-2-[[(thiophen-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
(2R,3R,4S,5R)-2-[(benzylamino)methyl]-5-(hydroxymethyl)pyrrolidine-3,4-diol
-
IC50 is 0.0062 mM
(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
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 2-fluorobenzoate
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 3-bromobenzoate
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-bromobenzoate
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-fluorobenzoate
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
(3S,4R)-pyrrolidine-3,4-diol
(6-butoxy-3-oxo-3,6-dihydro-2H-pyran-2-yl)methyl 2,2-dimethylpropanoate
-
-
(6-methoxy-3-oxo-3,6-dihydro-2H-pyran-2-yl)methyl 2,2-dimethylpropanoate
-
-
1,4-Dideoxy-1,4-imino-D-mannitol
-
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
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
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
1-cyclohexyl-3-(2-morpholinyl-4-ethyl)carbodiimide
-
inhibitory at 25 mM, pseudo-first-order kinetic
1-deoxy-mannojirimycin
-
complete inhibition
2-(2,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol
2-amino-2-deoxy-D-glucose
-
competitive inhibition, Ki = 2.8 mM
2-deoxy-2-fluoro-alpha-D-mannosyl fluoride
-
for mutant enzyme D341N, no inhibition of wild-type enzyme
3-bromo-N-[(2S)-2-[([(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl]benzamide
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
8,8a-di-epi-swainsonine
-
-
alpha-conglutin
-
11% inhibition at saturation
-
alpha-D-1,2-mannopyranosyl-mannopyranose
-
50% inhibition at 4 mM
alpha-D-1,3-mannopyranosyl-alpha-D-mannopyranose
-
50% inhibition at 18 mM
alpha-D-1,6-mannopyranosyl-mannopyranose
-
50% inhibition at 100 mM
cysteine
-
31% inhibition at 0.02 mM
D-glucose
-
67% inhibition at 30 mM
D-glucuronic acid
-
slight inhibition at 10 mM
D-mannono-gamma-lactone
-
-
diisopropylfluorophosphate
-
42% inhibition at 10 mM
EGTA
-
32% inhibition at 5 mM
gluco-hydroxyiminolactam
-
-
iodoacetamide
-
slight inhibition at 1 mM
Li+
-
88% inhibition at 20 mM
Mannan
-
33% inhibition at 50 mM
mannose
-
relative inhibition of 67.8%, potent inhibitor, three concentrations of 10, 50, and 100 mM tested
methyl-alpha-D-glucoside
-
23% inhibition at 10 mM
methyl-alpha-D-lyxopyranosyl-(1'-2)-alpha-D-mannopyranoside
-
-
methyl-alpha-D-lyxopyranosyl-(1-2)-alpha-D-mannopyranoside
-
potent
methyl-alpha-D-mannopyranoside
methyl-alpha-mannoside
-
not
N-bromosuccinimide
-
N-bromosuccinimide modified inactivation, effect of Trp modification on enzyme activity
N-octyl-6-epi-valienamine
-
-
Na+
-
1 mM, weak, not at 10 mM
NaN3
-
slight inhibition at 0.1 mM
p-chloromercuribenzenesulfonic acid
p-nitrophenyl-alpha-D-mannopyranoside
-
substrate inhibition greater than 2 mM
SDS
-
85% inhibition at 0.05%, w/v
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
-
Sr2+
-
inhibition at 1 mM
ZnCl2
-
92% inhibition by 1 mM, 56% inhibition by 0.01 mM
[6-(3-methylbutoxy)-3-oxo-3,6-dihydro-2H-pyran-2-yl]acetonitrile
-
-
[6-(3-methylbutoxy)-3-oxo-3,6-dihydro-2H-pyran-2-yl]methyl 2,2-dimethylpropanoate
-
-
[[(3S,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)piperidin-2-ylidene]amino] N-(4-chlorophenyl)carbamate
-
-
(1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
-
-
(1S,2R,8R,8aR)-octahydroindolizine-1,2,8-triol
-
-
(2R,3R,4S)-2-(aminomethyl)pyrrolidine-3,4-diol
-
1 mM, 81% inhibition, competitive
(2R,3R,4S)-2-(aminomethyl)pyrrolidine-3,4-diol
-
1 mM, 51% inhibition
(2R,3R,4S)-2-([[(1R)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol
-
1 mM, 75% inhibition, competitive
(2R,3R,4S)-2-([[(1R)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol
-
1 mM, 39% inhibition
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
-
-
(2R,3R,4S)-2-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidine-3,4-diol
-
-
(2R,3R,4S)-2-([[(1S)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol
-
1 mM, 66% inhibition, competitive
(2R,3R,4S)-2-([[(1S)-1-hydroxyethyl]amino]methyl)pyrrolidine-3,4-diol
-
1 mM, 45% inhibition
(2R,3R,4S)-2-hydroxymethyl-pyrrolidine-3,4-diol
-
1 mM, 54% inhibition
(2R,3R,4S)-2-hydroxymethyl-pyrrolidine-3,4-diol
-
1 mM, 37% inhibition
(2R,3R,4S)-2-phenylaminomethyl-pyrrolidine-3,4-diol
-
1 mM, 92% inhibition, competitive
(2R,3R,4S)-2-phenylaminomethyl-pyrrolidine-3,4-diol
-
1 mM, 69% inhibition, competitive
(2R,3R,4S)-2-[(1-phenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol
-
1 mM, 66% inhibition, competitive
(2R,3R,4S)-2-[(1-phenyl-ethylamino)-methyl]-pyrrolidine-3,4-diol
-
1 mM, 48% inhibition
(2R,3R,4S)-2-[(cyclopentylamino)methyl]pyrrolidine-3,4-diol
-
1 mM, 60% inhibition
(2R,3R,4S)-2-[(cyclopentylamino)methyl]pyrrolidine-3,4-diol
-
1 mM, 53% inhibition
(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
(2R,3R,4S)-2-[([(1R)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol
-
potent and selective inhibition
(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
(2R,3R,4S)-2-[([(1S)-2-hydroxy-1-phenylethyl]amino)methyl]pyrrolidine-3,4-diol
-
-
(2R,3R,4S)-2-[[(1-benzyl-piperidin-4-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 55% inhibition
(2R,3R,4S)-2-[[(1-benzyl-piperidin-4-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 59% inhibition
(2R,3R,4S)-2-[[(2H-Imidazol-1-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 55% inhibition
(2R,3R,4S)-2-[[(2H-Imidazol-1-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 59% inhibition
(2R,3R,4S)-2-[[(furan-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 49% inhibition
(2R,3R,4S)-2-[[(furan-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 29% inhibition
(2R,3R,4S)-2-[[(thiophen-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 89% inhibition, competitive
(2R,3R,4S)-2-[[(thiophen-2-ylmethyl)-amino]-methyl]-pyrrolidine-3,4-diol
-
1 mM, 68% inhibition, competitive
(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
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 2-fluorobenzoate
-
-
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 3-bromobenzoate
-
79% inhibition at 1 mM
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 3-bromobenzoate
-
-
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-bromobenzoate
-
92% inhibition at 1 mM
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-bromobenzoate
-
-
(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
(2S)-2-[([(2R,3S,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl 4-fluorobenzoate
-
-
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
-
-
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)-1-methylpyrrolidin-2-one
-
-
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
-
-
(3R,4R,5R)-3,4-dihydroxy-5-([[(1R)-2-hydroxy-1-phenylethyl]amino]methyl)pyrrolidin-2-one
-
-
(3S,4R)-pyrrolidine-3,4-diol
-
1 mM, 70% inhibition
(3S,4R)-pyrrolidine-3,4-diol
-
1 mM, 40% inhibition
1-deoxymannojirimicin
-
hydrolysis of 4-methylumbelliferyl-alpha-D-mannnopyranoside, strong inhibition for enzymes I and II at 0.025 mM
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
1-deoxymannojirimicin
-
19% inhibition at 0.01 mM
1-deoxymannojirimicin
-
complete inhibition at 1 mM
1-deoxymannojirimicin
-
IC50 = 0.01 mM
1-deoxymannojirimicin
-
50% inhibition at 0.05 mM
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
1-deoxymannojirimycin
-
61% inhibition of the activity of the liver lysosomal fraction at pH 4.0, 37% at pH 6.5, at 1 mM
1-deoxymannojirimycin
-
class 1 alpha1,2-mannosidase inhibitor
1-deoxymannojirimycin
-
pretreatment with 1-deoxymannojirimycin protectes primary cultured mouse cortical neurons from Amyloid beta1-42 toxicity
1-deoxymannojirimycin
-
mannose analog, in vivo and in vitro; reversible (not by Ca2+)
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
1-deoxymannojirimycin
-
-
1-deoxymannojirimycin
-
-
2-(2,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol
-
1 mM, 81% inhibition, mixed type
2-(2,2-dihydroxy-ethyl)-pyrrolidine-3,4-diol
-
1 mM, 56% inhibition
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
3-bromo-N-[(2S)-2-[([(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]methyl)amino]-2-phenylethyl]benzamide
-
-
Ag+
-
-
Ag+
-
52% inhibition at 10 mM
Ag+
-
slight inhibition at 1 mM for isoforms I, II
Ag+
-
97% inhibition at 10 mM
Ag+
strong inhibitor at concentrations of 1 mM or 10 mM
Ag+
-
70% inhibition at 1 mM
Ag+
-
moderate inhibition at 1 mM
alpha-D-mannopyranose
-
55% inhibition at 30 mM
alpha-D-mannopyranose
-
competitive inhibition, Ki: 22 mM
alpha-D-mannopyranose
-
29% inhibition at 10 mM
alpha-D-mannopyranose
-
27% inhibition at 10 mM
alpha-D-mannopyranose
-
competitive inhibition, Ki: 85 mM
alpha-D-mannopyranose
-
30% inhibition at 250 mM
alpha-D-mannopyranose
-
competitive inhibition, Ki: 20 mM
alpha-D-mannopyranose
-
50% inhibition at 250 mM
Ba2+
-
inhibition at 1 mM
Ba2+
-
10 mM; 78% inhibition at 10 mM
Ca2+
-
inhibition at 0.1 mM
Ca2+
-
inhibitory for enzyme I above 5 mM, enzyme II not affected
Ca2+
-
53% inhibition at 0.1 mM
Ca2+
-
slight inhibition at 1 mM
Cd2+
-
inhibition at 0.1 mM
Cd2+
-
10 mM, activation at 1 mM; 54% inhibition at 10 mM, slight stimulation at 1 mM
Co2+
-
51% inhibition at 10 mM
Co2+
-
slight inhibition at 10 mM
Co2+
-
46% inhibition at 1 mM
Co2+
-
10-30% inhibition for acid alpha-mannosidase
Co2+
-
slight inhibition at 1 mM
Co2+
-
inhibition of alpha-mannosidases IA and IB
Co2+
-
57% inhibition at 1 mM
Cu2+
-
87% inhibition at 20 mM
Cu2+
-
inhibition at 0.1 mM
Cu2+
-
10 mM; 41% inhibition at 10 mM
Cu2+
-
slight inhibition at 10 mM
Cu2+
-
complete inhibition at 1 mM
Cu2+
-
slight inhibition at 0.1 mM
Cu2+
-
nearly complete inhibition at 0.005 mM
Cu2+
-
complete inhibition at 0.1 mM
Cu2+
-
complete inhibition of the Co2+ activated enzyme at 0.5 mM
Cu2+
-
complete inhibition at 1 mM
Cu2+
-
10% inhibition at 10 mM, alpha-mannosidase A
Cu2+
strong inhibitor at concentrations of 1 mM or 10 mM
Cu2+
-
strong inhibition at 1 mM
Cu2+
-
inhibition of alpha-mannosidases IA, IB and II
Cu2+
-
strong inhibition at 1 mM
Cu2+
inhibits in presence of Co2+
Cu2+
-
nearly complete inhibition at 0.01 mM
D-mannono-1,4-lactone
-
36% inhibition at 10 mM
D-mannono-1,4-lactone
-
competitive inhibition, Ki: 13 mM
D-mannono-1,4-lactone
-
11% inhibition at 10 mM
D-mannono-1,4-lactone
-
Ki: 23.8 mM
D-mannono-1,5-lactone
-
complete inhibition at 1 mM
D-mannono-1,5-lactone
-
weak inhibition
D-mannono-1,5-lactone
-
50% competitive inhibition at 0.073 mM
D-mannosylamine
-
15% competitive inhibition at 5 mM
D-mannosylamine
-
56% inhibition at 1 mM
D-mannosylamine
-
competitive inhibition, Ki = 0.007 mM
deoxymannojirimycin
-
-
deoxymannojirimycin
Drosophila sp. (in: flies)
-
-
deoxymannojirimycin
less effective compared with swainsonine, concentration of 100 microM
deoxymannojirimycin
-
DMJ 3
EDTA
-
slight inhibition at 1 mM
EDTA
-
slight inhibition at 1 mM
EDTA
-
addition of Zn2+ restores inhibitory effect; strong inhibition at 1 mM
EDTA
-
37% inhibition at 5 mM
EDTA
-
addition of Zn2+ restores inhibitory effect
EDTA
-
complete inhibition at 1 mM, addition of 1 mM Zn2+ fully restores activity for isoforms II, to 69% for isoforms I
EDTA
-
complete inhibition at 20 mM, activity recovered in the presence of Ca2+
EDTA
-
addition of Zn2+ restores inhibitory effect
EDTA
-
addition of Zn2+ restores inhibitory effect
EDTA
-
complete inhibition at 0.05 mM
EDTA
supplied in equimolar amounts or in excess, neutralizes also effect of resistance of ManA to heat inactivation
EDTA
-
strong inhibition at 1 mM
EDTA
-
inhibitory for alpha-mannosidases IA and IB
EDTA
-
addition of Zn2+ restores inhibitory effect
EDTA
-
strong inhibition at 1 mM
EDTA
-
1 mM, more than 90% inactivation
EDTA
-
addition of Zn2+ restores inhibitory effect
EDTA
-
addition of Zn2+ restores inhibitory effect
EDTA
-
60-75% inhibition at 4 mM, activity restored by addition of Ca2+
EDTA
-
complete inactivition, Zn2+ restores, Ca2+, Cd2+, Mg2+, Ni2+, Na+ or Cu2+ restore partly
Fe2+
-
22% inhibition at 20 mM
Fe2+
-
58% inhibition at 10 mM
Fe2+
-
slight inhibition at 10 mM
Fe2+
-
54% inhibition at 1 mM
Fe2+
-
complete inhibition at 1 mM
Fe2+
-
slight inhibition at 1 mM
Fe2+
-
nearly complete inhibition at 1 mM
Fe3+
-
inhibition at 1 mM
Fe3+
-
43% inhibition at 1 mM
Fe3+
strong inhibitor at concentrations of 1 mM or 10 mM
Hg2+
-
strong inhibitor
Hg2+
-
complete inhibition at 10 mM
Hg2+
-
complete inhibition at 1 mM
Hg2+
-
slight inhibition at 1 mM for isoforms I,II
Hg2+
-
45% inhibition at 10 mM
Hg2+
-
complete inhibition at 1 mM
iodoacetic acid
-
-
iodoacetic acid
-
slight inhibition at 1 mM
iodoacetic acid
-
slight inhibition at 0.1 mM
kifunensine
-
-
kifunensine
little inhibitory effect, concentration of 10 microM
kifunensine
-
Kif 2, docking studies with the crystal structure of human alpha-1,2-mannosidase complexed with kifunensine (PDB: 1FO3) as a template
kifunensine
-
class 1 alpha1,2-mannosidase inhibitor
methyl-alpha-D-mannopyranoside
-
20% inhibition at 10 mM
methyl-alpha-D-mannopyranoside
-
40-50% inhibition of acid alpha-mannosidase, neutral alpha-mannosidase not affected
methyl-alpha-D-mannopyranoside
-
41% inhibition at 10 mM
methyl-alpha-D-mannopyranoside
-
slight inhibitory for alpha-mannosidases IA and IB
methyl-alpha-D-mannopyranoside
-
37% inhibition at 0.1 mM
Mg2+
-
61% inhibition at 20 mM
Mg2+
-
inhibition at 1 mM
Mg2+
-
slight inhibition at 1 mM
Mn2+
-
inhibition at 1 mM
Mn2+
-
slight inhibition at 1 mM
Mn2+
-
slight inhibition at 1 mM
Mn2+
-
inhibitory for enzyme I above 5 mM, slightly inhibitory for enzyme II
Mn2+
-
58% inhibition at 0.1 mM
Mn2+
-
complete inhibition at 1 mM
Mn2+
-
slight inhibition at 1 mM
Mn2+
-
slight inhibition at 1 mM
Ni2+
strong inhibitor at concentrations of 1 mM or 10 mM
Ni2+
-
moderate inhibition at 1 mM
Ni2+
inhibits in presence of Co2+
p-chloromercuribenzenesulfonic acid
-
strong inhibition at 1 mM
p-chloromercuribenzenesulfonic acid
-
different inhibition rates for alpha-mannosidases IA, IB and II
p-chloromercuribenzenesulfonic acid
-
strong inhibition at 1 mM
p-chloromercuribenzenesulfonic acid
-
complete inhibition at 1 mM
p-chloromercuribenzenesulfonic acid
-
50% inhibition at 0.35 mM, activity is restored by addition of substrate
Pb2+
-
complete inhibition of the Co2+ activated enzyme at 0.5 mM
Pb2+
-
moderate inhibition at 1 mM
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
swainsonine
-
IC50 is 400 nM
swainsonine
-
hydrolysis of 4-umbelliferyl-alpha-D-mannopyranoside, strong inhibition for enzymes I and II at 0.025 mM
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
swainsonine
-
swainsonine treatment completely inhibits the acid enzyme form activity below pH 5.0
swainsonine
-
complete inhibition of the Co2+ activated enzyme at 0.01 mM
swainsonine
-
IC50: 0.00011 mM
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
swainsonine
-
20% inhibition of glioblastoma cell growth at 0.25 mM
swainsonine
concentration of 100 microM
swainsonine
IC50: 0.00015 mM
swainsonine
shows competitive inhibition when p-nitrophenyl-Man is used as a substrate
swainsonine
-
competitive inhibition, Ki: 0.00036 mM
swainsonine
-
inhibition of both Tris-eluted and unbound isoforms from cobalt-chelating Sepharose, unbound: Ki: 0.028 mM, Tris-eluted: Ki: 0.004 mM
swainsonine
-
50% inhibition in the range of 0.3-0.6 mM
swainsonine
the enzyme substituted with Zn2+ is considerably less sensitive to swainsonine compared with the Co2+-, Cd2+-, and Mn2+-substituted enzyme
swainsonine
-
complete inhibition
swainsonine
-
IC50: 10 nM
swainsonine
binding structure, overview
swainsonine
-
competitive
swainsonine
-
competitive inhibition
swainsonine
-
50% inhibition at 0.00024 mM
swainsonine
-
complete inhibition at 0.008 mM
swainsonine
-
complete inhibition
Tris
-
in vivo and in vitro
Tris
-
inhibitory for alpha-mannosidases IA and IB
Zn2+
-
25% inhibition at 20 mM
Zn2+
-
inhibition at 1 mM
Zn2+
-
55% inhibition at 10 mM
Zn2+
-
complete inhibition of the Co2+ activated enzyme at 0.5 mM
Zn2+
-
complete inhibition at 1 mM
Zn2+
-
reversible by Ca2+
Zn2+
-
strong inhibition at 1 mM
Zn2+
-
slight inhibition for alpha-mannosidase IA
Zn2+
-
moderate inhibition at 1 mM
Zn2+
mutant enzymes H228Q, H533E, and H533Q, are all inhibited by high Zn2+ concentrations (1 mM)
additional information
-
no inhibition by L-cysteine
-
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
-
additional information
-
not inhibitory: 1,5-D-mannoseptanosyl di- and trisaccharide ring-size isomers
-
additional information
-
inhibition of growth of glioblastoma and melanoma cells by pyrrolidine-3,4-diol derivatives, overview
-
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
-
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
-
additional information
-
inhibitory activity of thiosugar derivatives (thiolevomannosans) is tested against alpha-mannosidase
-
additional information
-
no inhibition by Mg2+
-
additional information
1-deoxymannojirimycin has no effect on ManA at concentrations up to 500 microM
-
additional information
-
1-deoxymannojirimycin has no effect on ManA at concentrations up to 500 microM
-
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
-
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
-
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
-
additional information
-
no inhibition by 1-deoxymannojirimycin
-