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(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid
-
1-methyl cyclohexan bestatin
-
i.e. BE15, strong inhibition
2,4-dinitrofluorobenzene
-
-
2,6-pyridinedicarboxylate
-
-
2-Chloroethylphosphonic acid
-
-
3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]-propanoic acid
-
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
enzyme binding structure, overview
4-chloromercuribenzoate
-
-
5,5 dithiobis(2-nitrobenzoic acid)
-
1 mM, 74.89% enzyme inhibition
5,5'-dithiobis(2-nitrobenzoate)
Ag+
-
complete inhibition at 0.1 mM
Aprotinin
-
34% residual activity at 0.25 mg/ml
apstatin
0.1 mM, 50% inhibition
arginine derivatives
-
with carboxyl or alpha-amino group blocked
Borax-pyruvic acid buffer
-
-
citric acid-sodium citrate buffer
-
-
curcumin
-
non-competitive inhibitor
Cyclopeptide OF49-II
-
from Penicillium regulosum, total synthesis
-
DFP
5 mM, 25% inhibition. 10 mM, 44% inhibition
DX600
-
only blocks human ACE2 activity but not mouse
E-64
-
99% residual activity at 0.1 mM
Glu-pyrrolidide
0.1 mM, 98% inhibition
glutathione
-
high concentration
Gly-Gly
5 mM, 8% inhibition
HgCl2
-
complete inhibition at 1 mM
iodoacetate
-
0.1 mM, complete inactivation
kallidin
-
human peptide hormone, 10 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 73.7% (wild-type enzyme)
L-1-tosylamido-2-phenylethylchloromethylketone
-
-
L-Arg
5 mM, 70% inhibition
L-Arg-2-naphthylamide
-
competitive inhibition of hydrolysis of L-Ala-2-naphthylamide, no inhibition vice versa
L-Lys
5 mM, 28% inhibition
leuhistin
-
40% inhibition at 0.0003 mM, independent on TGF-beta1 activation
mangiferin
-
mixed non-competitive inhibitor
Mg2+
-
slight inhibition at 1 mM
MgCl2
-
0.1 mM MgCl2, 22% inhibition
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
-
N-alpha-p-Tosyl-L-lysine
-
-
N-alpha-p-tosyl-L-lysine-chloromethyl ketone
-
specific and irreversible inhibitor
N-[(2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl]-L-valyl-L-valyl-L-aspartic acid
-
-
N-[1-(R,S)-carboxy-3-phenyl propyl] Ala-Ala-Phe-p-aminobenzoate
-
-
Na+
-
NaCl (0.1-100 mM) has an opposite effect on the EGTA-treated KAP apo-enzyme, it inhibits 13% at 0.1 mM and 100% at 100 mM
NEM
-
13% inhibition at 1 mM
nitrobestatin
-
92.3% inhibition at 0.133 mM
o-phenanthroline
-
the native enzyme is inhibited by 76% at 0.5 mM, the recombinant enzyme is inhibited by 80% at 0.5 mM
p-aminophenylmercuric acetate
-
1 mM, 41.27% enzyme inhibition
p-chloromercuribenzene sulfonic acid
-
-
p-hydroxymercuriphenyl sulfonic acid
-
1 mM, 72.22% enzyme inhibition
p-Hydroxymercuriphenylsulfonic acid
-
-
PCMB
2 mM, complete inactivation
Phenylmethanesulfonylfluoride
suberanilohydroxamic acid
enzyme binding structure, overview
-
Substance P
-
human peptide hormone, 100 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 63.8% (wild-type enzyme); human peptide hormone, 10 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 78% (wild-type enzyme)
tert-butyl bestatin
-
i.e. BE17, the BE15 derivative has a dual inhibitory effect of invasion and motility on tumor and endothelial cells
[(2Z)-3-[(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)methyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
11.7% inhibition at 0.01 mM
[(2Z)-3-[2-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
54.8% inhibition at 0.01 mM
[(2Z)-3-[2-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
32.8% inhibition at 0.01 mM
[(2Z)-3-[2-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
53.5% inhibition at 0.01 mM
[(2Z)-3-[2-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
65.2% inhibition at 0.01 mM
[(2Z)-3-[2-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
36.4% inhibition at 0.01 mM
[(2Z)-3-[4-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
26.0% inhibition at 0.01 mM
[(2Z)-3-[4-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
22.2% inhibition at 0.01 mM
[(2Z)-3-[4-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
26.8% inhibition at 0.01 mM
[(2Z)-3-[4-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
33.7% inhibition at 0.01 mM
[(2Z)-3-[4-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
26.0% inhibition at 0.01 mM
[(2Z)-3-[5-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
52.6% inhibition at 0.01 mM
[(2Z)-3-[5-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
34.1% inhibition at 0.01 mM
[(2Z)-3-[5-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
78.8% inhibition at 0.01 mM
[(2Z)-3-[5-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
76.1% inhibition at 0.01 mM
[(2Z)-3-[5-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
54.0% inhibition at 0.01 mM
[(2Z)-3-[6-(5-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
37.8% inhibition at 0.01 mM
[(2Z)-3-[6-(6-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
68.8% inhibition at 0.01 mM
[(2Z)-3-[6-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
62.5% inhibition at 0.01 mM
[(2Z)-3-[6-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
36.9% inhibition at 0.01 mM
[(2Z)-3-[6-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
70.6% inhibition at 0.01 mM
[(2Z)-3-[6-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
80.6% inhibition at 0.01 mM
[(2Z)-3-[6-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
51.7% inhibition at 0.01 mM
[(2Z)-3-[6-(7-methoxy-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
50.3% inhibition at 0.01 mM
[(2Z)-3-[6-(7-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
34.6% inhibition at 0.01 mM
[(2Z)-3-[6-(8-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
37.9% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[(4-oxo-1,2,3-benzotriazin-3(4H)-yl)methyl]-1,3-thiazolidin-2-ylidene]cyanamide
over 10.0% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[2-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-1,3-thiazolidin-2-ylidene]cyanamide
30.2% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[2-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]ethyl]-1,3-thiazolidin-2-ylidene]cyanamide
55.6% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[4-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]butyl]-1,3-thiazolidin-2-ylidene]cyanamide
41.6% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[5-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]pentyl]-1,3-thiazolidin-2-ylidene]cyanamide
50.1% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[6-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]hexyl]-1,3-thiazolidin-2-ylidene]cyanamide
60.1% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]methyl]-1,3-thiazolidin-2-ylidene]cyanamide
15.8% inhibition at 0.01 mM
1,10-phenanthroline
-
-
1,10-phenanthroline
complete inhibition, reversible by Zn2+
1,10-phenanthroline
-
activity restored by Co2+
1,10-phenanthroline
effective
1,10-phenanthroline
-
reversible by Zn2+
1,10-phenanthroline
-
34% residual activity at 1 mM
1,10-phenanthroline
-
complete inhibition at 1 mM
1,10-phenanthroline
-
68.5% inhibition at 5 mM
2-mercaptoethanol
-
-
2-mercaptoethanol
-
enzyme II
3,4-dichloroisocoumarin
-
0.1 mM, 12% inhibition. 1.0 mM, 16% inhibition
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
2 mM, 38% inhibition
5,5'-dithiobis(2-nitrobenzoate)
-
-
5,5'-dithiobis(2-nitrobenzoate)
-
-
actinonin
-
40% inhibition at 0.0003 mM, independent on TGF-beta1 activation
amastatin
-
amastatin
-
50-70% inhibition at 0.0003 mM, dependent on TGF-beta1 activation
amastatin
1 mM, 11% inhibition
amino acids
-
-
Arg
-
noncompetitive
arphamenine A
complete inhibition at 0.1 mM
arphamenine A
-
aminopeptidase B-specific inhibitor
arphamenine A
-
the native enzyme is completely inhibited at 0.001 mM, the recombinant enzyme is completely inhibited at 0.001 mM
arphamenine A
-
complete inhibition at 0.1 mM
Arphamenine B
-
-
Arphamenine B
aminopeptidase B-specific inhibitor
Arphamenine B
-
the native enzyme is completely inhibited at 0.001 mM, the recombinant enzyme is completely inhibited at 0.001 mM
bestatin
-
-
bestatin
complete inhibition at 0.1 mM
bestatin
-
strong inhibition
bestatin
orally applicated inhibits the melanoma cell-induced angiogenesis in mice air sacs
bestatin
-
the native enzyme is completely inhibited at 0.05 mM, the recombinant enzyme is completely inhibited at 0.1 mM
bestatin
-
complete inhibition at 0.1 mM
bestatin
-
highly sensitive to bestatin
bestatin
1 mM, 32% inhibition
bestatin
-
84.8% inhibition at 0.3 mM
beta-mercaptoethanol
4% inhibition at 10 mM
beta-mercaptoethanol
-
20% inhibition at 10 mM
Ca2+
-
16% inhibition at 1 mM, 24% inhibition at 10 mM
Ca2+
-
0.1 mM CaCl2, 19% inhibition
Ca2+
-
19% inhibition at 1 mM
Ca2+
-
slight inhibition at 1 mM
Cd2+
-
-
Cd2+
-
inhibits Cd2+-saturated enzyme, inhibits the Ni2+-saturated enzyme
Cd2+
-
complete inhibition at 1 mM
Co2+
62% inhibition at 1 mM
Co2+
-
inhibits Cd2+-saturated enzyme, inhibits the Ni2+-saturated enzyme
Co2+
-
0.1 mM CoCl2, 23% inhibition
Co2+
-
45% inhibition at 1 mM
Co2+
-
76% inhibition at 1 mM
Co2+
-
strong inhibition at 1 mM
Cu2+
-
84% inhibition at 0.1 mM
Cu2+
-
0.1 mM CuCl2, complete inhibition
Cu2+
-
complete inhibition at 1 mM
Cu2+
-
complete inhibition at 1 mM
cysteine
21% inhibition at 1 mM
cysteine
-
15% inhibition at 1 mM
dithiothreitol
33% inhibition at 10 mM
dithiothreitol
-
54% inhibition at 10 mM
DTT
-
1 mM, complete inhibition of enzyme activity
DTT
-
25% inhibition at 1 mM, complete inhibition at 10 mM
DTT
-
9% inhibition at 1 mM
E64
48% inhibition at 0.01 mM
E64
-
12% inhibition at 0.01 mM
EDTA
12% inhibition at 1 mM
EDTA
-
1 mM, 42.33% enzyme inhibition
EDTA
-
complete inhibition at 1-10 mM
EDTA
-
complete loss of activity after dialysis with EDTA
EDTA
-
the native enzyme is inhibited by 95% at 10 mM, the recombinant enzyme is inhibited by 71% at 10 mM
EDTA
-
54% inhibition at 1 mM
EDTA
-
61% residual activity at 1 mM
EDTA
-
90% inhibition at 1 mM
EGTA
-
-
EGTA
-
complete inhibition at 1 mM
Fe2+
-
-
Fe2+
-
inhibits the Ni2+-saturated enzyme
Hg2+
-
complete inhibition at 0.1 mM
Hg2+
-
0.1 mM HgCl2, complete inhibition
Hg2+
-
complete inhibition at 1 mM
Hg2+
-
complete inhibition at 1 mM
iodoacetamide
5 mM, 9% inhibition
iodoacetamide
-
16% inhibition at 1 mM
leupeptin
-
5% inhibition at 0.01 mM
Lys
-
noncompetitive
MLN-4760
-
MLN-4760 inhibits both human and mouse ACE2
MLN-4760
-
MLN-4760 inhibits both human and mouse ACE2
Mn2+
-
complete inhibition at 10 mM
Mn2+
-
82% inhibition at 1 mM
Mn2+
-
strong inhibition at 1 mM
N-ethylmaleimide
44% inhibition at 0.1 mM
N-ethylmaleimide
-
the native enzyme is inhibited by 45% at 1 mM, the recombinant enzyme is inhibited by 71% at 1 mM
N-ethylmaleimide
-
21% inhibition at 0.1 mM
NaI
-
-
Ni2+
75% inhibition at 1 mM
Ni2+
-
inhibits Cd2+-saturated enzyme
Ni2+
-
63% inhibition at 1 mM
Ni2+
-
complete inhibition at 1 mM
Ni2+
-
strong inhibition at 1 mM
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
Pb2+
-
-
Pb2+
-
84% inhibition at 1 mM
pefabloc
5 mM, 60% inhibition. 10 mM 69% inhibition
pepstatin
-
93% residual activity at 0.1 mM
pepstatin
-
5% inhibition at 0.01 mM
Phenylmethanesulfonylfluoride
10% inhibition at 0.1 mM
Phenylmethanesulfonylfluoride
-
1% inhibition at 0.1 mM
Phenylmethanesulfonylfluoride
-
45% residual activity at 0.5 mM
PMSF
-
14% inhibition at 1 mM
puromycin
-
-
puromycin
10% inhibition at 0.1 mM
puromycin
-
1% inhibition at 0.1 mM
SDS
5%, 96% inhibition
Urea
2 M, 18% inhibition
Zn2+
complete inhibition at 0.1 mM
Zn2+
-
complete inhibition at 0.1-10 mM
Zn2+
-
inhibits Cd2+-saturated enzyme, inhibits the Ni2+-saturated enzyme
Zn2+
-
0.1 mM ZnCl2, 82% inhibition
Zn2+
-
99% inhibition at 0.1 mM
Zn2+
-
80% inhibition at 1 mM
Zn2+
-
Zn2+ inhibits AP-B reversibly at micromolar concentrations (0.005-0.05 mM), AP-B with 0.25 Zn2+ becomes susceptible to degradation by trypsin suggesting that Zn2+ alters enzyme conformation, complete inhibition occurs at 0.050-0.080 mM
Zn2+
-
complete inhibition at 1 mM
ZnCl2
-
-
ZnCl2
-
96% inhibition at 1 mM
additional information
-
no inhibition at 0.1 mM by Mg2+
-
additional information
EDTA has no effect up to 1 mM
-
additional information
-
EDTA has no effect up to 1 mM
-
additional information
-
inhibitory potency of bestatin and derivatives on enzyme activity, umbilical vein endothelial cell vessel formation, and cell invasion and migration, overview
-
additional information
synthesis and evaluation of a series of 1,2,3-benzotriazin-4-one derivatives as inhibitors of leukotriene A4 hydrolase aminopeptidase activity of the enzyme in vitro, overview. Molecular docking and structure-activity relationship of the inhibitors, IC50 values for cytotoxic effects on THP-1 cells
-
additional information
drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modeling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
-
additional information
-
no or poor inhibition of L-Arg-2-naphthylamide hydrolysis by puromycin at 1 mM, aprotinin, pepstatin A, E64, chymostatin, imipramine, phosphoramidon, lisinopril, and apstatin
-
additional information
-
no inhibition by PMSF, pepstatin, and aprotinin
-
additional information
-
no inhibition by puromycin
-
additional information
-
no inhibition by PMSF, pepstatin, and aprotinin
-
additional information
-
not affected by phenylmethylsulfonylfluoride
-
additional information
-
insensitive to L-Arg-hydroxamate, L-Lys-hydroxamate, puromycin, and amastatin
-
additional information
-
At 0.2 mM, no significant inhibitory effect is observed with caffeic, chlorogenic, ferulic, salicylic and sinapic acids as well as with resveratrol
-
additional information
-
no inhibition by phosphoramidon, E64, antipaine, and TLCK
-
additional information
-
no inhibition by pepstatin
-
additional information
-
no inhibition by epibestatin, and by E64, chymostatin, leupeptin, and antipain
-