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11-aminoundecanoic acid
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2,2'-bipyridine
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5.0 mM, 29% inhibition
2,9-Dimethyl-1,10-phenanthroline
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2.0 mM, 52% inhibition
6-aminopenicillanic acid
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-
8-hydroxyquinoline
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2.0 mM, 84% inhibition
acetonitrile
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20% complete loss of activity
actinonin
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0.1 mM, complete inactivation
Ala-Ala
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inhibits hyrolysis of Ala-2-naphthylamide
Ala-Ala-Ala
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inhibits hyrolysis of Ala-2-naphthylamide
Ala-Ala-Ala-Ala
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inhibits hyrolysis of Ala-2-naphthylamide
Ala-Ala-Phe-chloromethyl ketone
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anti-PSA immunglobulinb G
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53.4% residual activity at 0.1 mg/ml
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antipain
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0.1 mM, 39% inhibition
Aprotinin
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82% residual activity at 0.1 mM
arphamenine A
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0.1 mM, 80% inactivation
azide
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92% inhibition at 10 mM
benzamidine
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1 mM, 14% inhibition
benzylpenicillenic acid
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-
benzylpenicilloic acid
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-
Cd2+
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1 mM, complete inhibition
CdCl2
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6.2% residual activity at 1 mM
chymostatin
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0.1 mM, 83% inhibition
Co2+
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1 mM, complete inhibition
Cu2+
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1 mM, complete inhibition
CuSO4
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0.6% residual activity at 1 mM
cyanide
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84% inhibition at 10 mM
E-64
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27.2% residual activity at 0.015 mM
ethanol
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inactivation above 30%
Gly-Gly-Ala
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inhibits hyrolysis of Ala-4-nitroanilide
Gly-Gly-Phe
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inhibits hyrolysis of Ala-4-nitroanilide
iodoacetamide
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1 mM, 57% inhibition
iodoacetic acid
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1 mM, 11% inhibition
KCN
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10 mM, 84% inhibition
L-arginine
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19.3% residual activity at 5 mM
L-cysteine
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non-competitive, 7.3% residual activity at 5 mM
L-isoleucine
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20.1% residual activity at 5 mM
L-leucine
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6.9% residual activity at 5 mM
L-phenylalanine
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21.1% residual activity at 5 mM
L-tryptophan
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15.5% residual activity at 5 mM
L-valine
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23.7% residual activity at 5 mM
Leu
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noncompetitive with Ala-2-naphthylamide, mixed type inhibition with Leu-Leu-Leu, competitive inhibition with Ala-Ala-Ala
leuhistin
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0.1 mM, complete inactivation
Met
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noncompetitive with Ala-2-naphthylamide
Met-NH2
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competitive with Ala-2-naphthylamide
methanol
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inactivation only above 30%
Methyl cellosolve
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40% loss of activity at 40% solvent
Mg2+
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1 mM, 20% inhibition
Mn2+
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1 mM, 69% inhibition
Na2S
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10 mM, 92% inhibition
NaCl
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hydrolysis of Ala-4-nitropanilide, competitive inhibition at pH 6.6, inhibition is noncompetitive at pH 5.8, inhibition is mixed type at pH 6.2
NEM
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1 mM, 43% inhibition
Ni2+
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1 mM, 90% inhibition
octanoic acid
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competitive
oxalate
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50 mM ammonium oxalate, 71% inhibition
p-dioxane
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inactivation only above 30%
phosphoramidon
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0.1 mM, 17% inhibition
PMSF
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1 mM, 40% inhibition; 1 mM, 64% inhibition
puromycin aminonucleoside
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-
Tyr
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noncompetitive with Ala-2-naphthylamide, competitive with Ala-Ala-Ala
ZnSO4
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24% residual activity at 1 mM
1,10-phenanthroline
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19.4% residual activity at 0.2 mM
1,10-phenanthroline
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99% inhibition at 0.5 mM; Ki 0.028 mM
1,10-phenanthroline
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1 mM, complete inhibition
amastatin
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-
amastatin
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0.1 mM, complete inactivation
bestatin
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1.1% residual activity at 0.05 mM
bestatin
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2.57% residual activity at 0.1 mM
bestatin
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0.1 mM complete inactivation
EDTA
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17.5% residual activity at 5 mM, 3,3% residual activity after extensively dialysis against 1 mM, restored by 0.01 mM Zn2+ to 57.8% activity
EDTA
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98% inhibition at 0.001 mM
EDTA
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44% residual activity at 0.5 mM
EDTA
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2 mM, 26% inhibition
EGTA
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24.3% residual activity at 5 mM
EGTA
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96% inhibition at 1 mM; Ki 0.012 mM
Leu-Leu-Leu
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-
Leu-Leu-Leu
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inhibits hyrolysis of Ala-2-naphthylamide
leupeptin
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83% residual activity at 0.1 mM
leupeptin
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0.1 mM, 19% inhibition
Phe
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-
Phe
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noncompetitive with Ala-2-naphthylamide
puromycin
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9.5% residual activity at 0.01 mM
puromycin
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3.12% residual activity at 0.1 mM
puromycin
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0.1 mM, complete inactivation, IC50: 0.0006 mM
Zn2+
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79.4% residual activity at 0.01 mM
Zn2+
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1 mM, complete inhibition
additional information
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there are two active centre ionizable groups with pKa values of approximately 6.0 and 7.5 which are involved in substrate binding or inhibitory amino acid binding
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additional information
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not inhibited by phenylmethylsulfonylfluoride
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additional information
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D-glucose and insulin do not alter enzyme activity
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3.4.11.14 cytosol alanyl aminopeptidase
results (
results (
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