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Ala-2-naphthylamide + H2O
Ala + 2-naphthylamine
-
-
-
-
?
Ala-4-nitroanilide + H2O
Ala + 4-nitroaniline
-
4.6% of the activity with Leu-4-nitroanilide
-
?
Ala-Ala 4-nitroanilide + H2O
Ala-Ala + 4-nitroaniline
alpha-Glu-4-nitroanilide + H2O
Glu + 4-nitroaniline
-
564% of the activity with Leu-4-nitroanilide
-
?
angiotensin III + H2O
angiotensin IV + ?
-
-
-
-
?
Arg 4-methylcoumarin 7-amide + H2O
Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Arg-4-methylcoumarin 7-amide + H2O
Arg + 7-amino-4-methylcoumarin
Arg-4-methylcoumaryl-7-amide + H2O
Arg + 7-amino-4-methylcoumarin
-
-
?
Arg-4-nitroanilide + H2O
Arg + 4-nitroaniline
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
Arg-Ala + H2O
Arg + Ala
-
82% of the activity with Arg-Arg
-
?
Arg-alpha-atrial natriuretic factor1-20 + H2O
Arg + alpha-atrial natriuretic factor1-20
-
-
-
-
?
Arg-Arg + H2O
Arg + Arg
-
-
-
?
Arg-Asp + H2O
Arg + Asp
-
25% of the activity with Arg-Arg
-
?
Arg-beta-atrial natriuretic factor1-20 + H2O
Arg + beta-atrial natriuretic factor1-20
-
-
-
-
?
Arg-beta-naphthylamide + H2O
L-arginine + 2-naphthylamine
-
substrate used in the activity assay
-
-
?
Arg-Gly + H2O
Arg + Gly
-
-
?
Arg-Gly-Asp-Ser-Pro-Ala-Ser-Ser-Lys-Pro + H2O
Arg + Gly-Asp-Ser-Pro-Ala-Ser-Ser-Lys-Pro
i.e. fibronectin-binding inhibitor
-
?
Arg-Gly-Glu-Ser + H2O
Arg + Gly-Glu-Ser
i.e. platelet aggregation inhibitor
-
?
Arg-Gly-Pro-Phe-Pro-Ile + H2O
Arg + Gly-Pro-Phe-Pro-Ile
i.e. sexual agglutination peptide
-
?
Arg-Gly-Tyr-Ala-Leu-Gly + H2O
Arg + Gly-Tyr-Ala-Leu-Gly
-
-
-
-
?
Arg-Ile + H2O
Arg + Ile
-
32% of the activity with Arg-Arg
-
?
Arg-Leu + H2O
Arg + Leu
-
25% of the activity with Arg-Arg
-
?
Arg-Leu-enkephalin + H2O
Arg + Leu-enkephalin
-
-
-
-
?
Arg-Lys + H2O
Arg + Lys
-
88% of the activity with Arg-Arg
-
?
Arg-Lys-Asp-Val-Tyr-OH + H2O
?
-
-
-
-
?
Arg-Lys-somatostatin-14 + H2O
Arg + Lys + somatostatin-14
-
sequential removal of basic N-terminal residues
-
-
?
Arg-Lys-somatostatin-14 + H2O
Arg-Lys + somatostatin-14
-
-
-
-
?
Arg-Met-enkephalin + H2O
?
-
-
-
-
?
Arg-Met-enkephalin + H2O
Arg + Met-enkephalin
-
-
-
-
?
Arg-neurokinin A + H2O
Arg + neurokinin A
-
-
-
-
?
Arg-Phe-Ala-Arg-Lys-Gly-Ala-Leu-Arg-Gln-Lys-Asn-Val + H2O
Arg + Phe-Ala-Arg-Lys-Gly-Ala-Leu-Arg-Gln-Lys-Asn-Val
i.e. protein kinase C substrate
-
?
Arg-Pro-Lys-Pro-Gln-Gly-Leu-Met + H2O
Arg + Pro-Lys-Pro-Gln-Gly-Leu-Met
i.e. substance P
-
?
Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg + H2O
Arg + Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg
Arg-Tyr-Leu-Pro-Thr + H2O
Arg + Tyr-Leu-Pro-Thr
-
proctolin
-
-
?
Arg-Val-Tyr-Ile-His-Pro-Ile + H2O
Arg + Val-Tyr-Ile-His-Pro-Ile
i.e. angiotensin III
-
?
Arg-Val-Tyr-Ile-His-Pro-Phe + H2O
Arg + Val-Tyr-Ile-His-Pro-Phe
-
angiotensin III
-
-
?
azocasein + H2O
?
-
-
-
-
?
azocasein + H2O
protein fragments of azocasein of MW 71 kDa, 83 kDa, and 22 kDa
-
-
-
-
?
benzoyl-Arg-p-nitroanilide + H2O
benzoyl-Arg + p-nitroaniline
-
-
-
-
?
Cys-Gly + H2O
Cys + Gly
-
4210% of the activity with Leu-4-nitroanilide
-
?
elastin Congo red + H2O
?
-
-
-
-
?
glucagon + H2O
miniglucagon + ?
-
-
-
-
?
Gly-2-naphthylamide + H2O
Gly + 2-naphthylamine
Gly-4-nitroanilide + H2O
Gly + 4-nitroaniline
-
1.3% of the activity with Leu-4-nitroanilide
-
?
Gly-L-Pro-2-naphthylamide + H2O
Gly-L-Pro + 2-naphthylamine
-
1% activity compared to L-Lys-2-naphthylamide
-
-
?
Gly-Phe 4-nitroanilide + H2O
Gly-Phe + 4-nitroaniline
kallidin + H2O
?
-
-
-
-
?
kallidin + H2O
bradykinin + ?
i.e. KRPPGFSPFR
-
-
?
kallidin-10 + H2O
Lys + bradykinin
-
-
-
-
?
L-Ala-2-naphthylamide + H2O
L-Ala + 2-naphthylamine
L-Ala-4-nitroanilide + H2O
L-Ala + 4-nitroaniline
L-Ala-7-amido-4-methylcoumarin + H2O
L-Ala + 7-amino-4-methylcoumarin
L-Ala-Ala-Pro-Leu-4-nitroanilide + H2O
L-Ala-Ala-Pro-Leu + 4-nitroaniline
-
-
-
-
?
L-Arg 7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
fluorogenic substrate, best substrate
-
-
?
L-Arg-(Met)enkephalin + H2O
L-Arg + (Met)enkephalin
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
L-Arg-4-nitroanilide + H2O
L-Arg + 4-nitroaniline
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
L-Arg-L-Tyr-Gly-Gly-L-Phe-L-Leu + H2O
L-Arg + L-Tyr-Gly-Gly-L-Phe-L-Leu
-
-
-
-
?
L-Arg-p-nitroanilide + H2O
L-Arg + p-nitroaniline
L-Arg-peptide + H2O
L-Arg + peptide
-
specific for N-terminal Arg or Lys residues, di-, tri-, and polypeptides
-
-
?
L-arginine-2-naphthylamide + H2O
2-naphthylamine + L-Arg
-
assay at 37°C
-
-
?
L-Asn-7-amido-4-methylcoumarin + H2O
L-Asn + 7-amino-4-methylcoumarin
53% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Asp-7-amido-4-methylcoumarin + H2O
L-Asp + 7-amino-4-methylcoumarin
15% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-beta-Asn-2-naphthylamide + H2O
L-beta-Asn + 2-naphthylamine
-
9% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Cys-2-naphthylamide + H2O
L-Cys + 2-naphthylamine
-
1% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Cys-7-amido-4-methylcoumarin + H2O
L-Cys + 7-amino-4-methylcoumarin
-
5% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Gln-7-amido-4-methylcoumarin + H2O
L-Gln + 7-amino-4-methylcoumarin
about 1% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Gly-L-Arg-2-naphthylamide + H2O
L-Gly-L-Arg + 2-naphthylamine
-
250% activity compared to L-Lys-2-naphthylamide
-
-
?
L-His-2-naphthylamide + H2O
L-His + 2-naphthylamine
-
15% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Ile-7-amido-4-methylcoumarin + H2O
L-Ile + 7-amino-4-methylcoumarin
about 1% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Leu 7-amido-4-methylcoumarin + H2O
L-Leu + 7-amino-4-methylcoumarin
-
fluorogenic substrate
-
-
?
L-Leu-2-naphthylamide + H2O
L-Leu + 2-naphthylamine
L-Leu-4-nitroanilide + H2O
L-Leu + 4-nitroaniline
L-Leu-7-amido-4-methylcoumarin + H2O
L-Leu + 7-amino-4-methylcoumarin
L-Lys-(Met)enkephalin + H2O
L-Lys + (Met)enkephalin
L-Lys-2-naphthylamide + H2O
L-Lys + 2-naphthylamine
L-Lys-4-nitroanilide + H2O
L-Lys + 4-nitroaniline
L-Lys-7-amido-4-methylcoumarin + H2O
L-Lys + 7-amino-4-methylcoumarin
L-Lys-L-Ala-2-naphthylamide + H2O
L-Lys-L-Ala + 2-naphthylamine
-
7% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Lys-p-nitroanilide + H2O
L-Lys + p-nitroaniline
-
-
-
-
?
L-Lys-peptide + H2O
L-Lys + peptide
-
specific for N-terminal Arg or Lys residues, di-, tri-, and polypeptide
-
-
?
L-lysine-2-naphthylamide + H2O
2-naphthylamine + L-Lys
-
assay at 37°C
-
-
?
L-Met-2-naphthylamide + H2O
L-Met + 2-naphthylamine
L-Met-7-amido-4-methylcoumarin + H2O
L-Met + 7-amino-4-methylcoumarin
L-Phe-2-naphthylamide + H2O
L-Phe + 2-naphthylamine
-
0.171% activity compared to L-Arg-2-naphthylamide
-
-
?
L-Phe-7-amido-4-methylcoumarin + H2O
L-Phe + 7-amino-4-methylcoumarin
L-Pro-7-amido-4-methylcoumarin + H2O
L-Pro + 7-amino-4-methylcoumarin
-
7% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Ser-7-amido-4-methylcoumarin + H2O
L-Ser + 7-amino-4-methylcoumarin
15% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Tyr 7-amido-4-methylcoumarin + H2O
L-Tyr + 7-amino-4-methylcoumarin
-
fluorogenic substrate
-
-
?
L-Tyr-2-naphthylamide + H2O
L-Tyr + 2-naphthylamine
L-Tyr-7-amido-4-methylcoumarin + H2O
L-Tyr + 7-amino-4-methylcoumarin
about 7% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Val-2-naphthylamide + H2O
L-Val + 2-naphthylamine
-
0.034% activity compared to L-Arg-2-naphthylamide
-
-
?
L-Val-4-nitroanilide + H2O
L-Val + 4-nitroaniline
low activity
-
-
?
L-Val-7-amido-4-methylcoumarin + H2O
L-Val + 7-amino-4-methylcoumarin
about 1% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
Leu-2-naphthylamide + H2O
Leu + 2-naphthylamine
-
-
-
-
?
Leu-4-nitroanilide + H2O
Leu + 4-nitroaniline
Leu-Gly + H2O
Leu + Gly
-
1200% of the activity with Leu-4-nitroanilide
-
?
leukotriene A4 + H2O
L-Arg + leukotriene B4
-
weak in vitro activity
-
-
?
leukotriene A4 + H2O
leukotriene B4 + ?
-
has a residual catalytic ability to hydrolyze leukotriene A4
-
-
?
Lys 4-methylcoumarin 7-amide + H2O
Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
Lys-2-naphthylamide + H2O
Lys + 2-naphthylamine
Lys-4-methylcoumarin 7-amide + H2O
Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
Lys-4-nitroanilide + H2O
Lys + 4-nitroaniline
Lys-7-amido-4-methylcoumarin + H2O
Lys + 7-amino-4-methylcoumarin
-
4.3% of the activity with Arg-7-amido-4-methylcoumarin
-
?
Lys-Ala + H2O
Lys + Ala
-
88% of the activity with Arg-Arg
-
?
Lys-Leu-2-naphthylamide + H2O
Lys + Leu-2-naphthylamide
-
-
-
-
?
Lys-Lys + H2O
Lys + Lys
-
30% of the activity with Arg-Arg
-
?
Met-4-nitroanilide + H2O
Met + 4-nitroaniline
-
40.6% of the activity with Leu-4-nitroanilide
-
?
Met-enkephalin + H2O
?
-
-
-
-
?
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
N-p-tosyl-Gly-Pro-Lys + p-nitroaniline
-
-
-
-
?
N-succinyl-Gly-Pro-Leu-Gly-Pro 7-amido-4-methylcoumarin + H2O
N-succinyl-Gly-Pro-Leu-Gly-Pro + 7-amino-4-methylcoumarin
-
fluorogenic substrate
-
-
?
Poly-L-lysine + H2O
?
-
-
-
-
?
thymopentin + H2O
?
-
-
-
-
?
Val-4-nitroanilide + H2O
Val + 4-nitroaniline
-
1.2% of the activity with Leu-4-nitroanilide
-
?
[Arg0]-Met-enkephalin + H2O
Met-enkephalin + de-[Tyr]-Met-enkephalin
i.e. RYGGFM
-
-
?
additional information
?
-
Ala-Ala 4-nitroanilide + H2O

Ala-Ala + 4-nitroaniline
-
-
-
?
Ala-Ala 4-nitroanilide + H2O
Ala-Ala + 4-nitroaniline
-
-
-
?
Arg-4-methylcoumarin 7-amide + H2O

Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Arg-4-methylcoumarin 7-amide + H2O
Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Arg-4-nitroanilide + H2O

Arg + 4-nitroaniline
-
2.5% of the activity with Leu-4-nitroanilide
-
?
Arg-4-nitroanilide + H2O
Arg + 4-nitroaniline
-
as active as Arg-7-amido-4-methylcoumarin
-
?
Arg-4-nitroanilide + H2O
Arg + 4-nitroaniline
-
-
?
Arg-7-amido-4-methylcoumarin + H2O

Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
-
-
-
?
Arg-peptides + H2O

?
-
-
-
-
?
Arg-peptides + H2O
?
-
or Lys-peptides, metabolism of kinin
-
-
?
Arg-peptides + H2O
?
-
attribution to inflammatory and wound healing processes
-
-
?
Arg-peptides + H2O
?
-
takes part in later stages of protein degradation in chloroplasts
-
-
?
Arg-peptides + H2O
?
-
-
-
-
?
Arg-peptides + H2O
?
-
-
-
-
?
Arg-Phe + H2O

Arg + Phe
-
35% of the activity with Arg-Arg
-
?
Arg-Phe + H2O
Arg + Phe
-
-
?
Arg-Pro + H2O

Arg + Pro
-
-
?
Arg-Pro + H2O
Arg + Pro
-
-
?
Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg + H2O

Arg + Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg
i.e. bradykinin
-
?
Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg + H2O
Arg + Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg
i.e. bradykinin
-
?
Gly-2-naphthylamide + H2O

Gly + 2-naphthylamine
-
1% activity compared to L-Lys-2-naphthylamide
-
-
?
Gly-2-naphthylamide + H2O
Gly + 2-naphthylamine
-
less than 0.02% activity compared to L-Arg-2-naphthylamide
-
-
?
Gly-Phe 4-nitroanilide + H2O

Gly-Phe + 4-nitroaniline
-
-
-
?
Gly-Phe 4-nitroanilide + H2O
Gly-Phe + 4-nitroaniline
-
-
-
?
L-Ala-2-naphthylamide + H2O

L-Ala + 2-naphthylamine
-
-
-
-
?
L-Ala-2-naphthylamide + H2O
L-Ala + 2-naphthylamine
-
-
-
-
?
L-Ala-2-naphthylamide + H2O
L-Ala + 2-naphthylamine
-
0.1% activity compared to L-Arg-2-naphthylamide
-
-
?
L-Ala-2-naphthylamide + H2O
L-Ala + 2-naphthylamine
-
83% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Ala-4-nitroanilide + H2O

L-Ala + 4-nitroaniline
low activity
-
-
?
L-Ala-4-nitroanilide + H2O
L-Ala + 4-nitroaniline
-
-
-
-
?
L-Ala-4-nitroanilide + H2O
L-Ala + 4-nitroaniline
-
-
-
-
?
L-Ala-7-amido-4-methylcoumarin + H2O

L-Ala + 7-amino-4-methylcoumarin
-
best substrate
-
-
?
L-Ala-7-amido-4-methylcoumarin + H2O
L-Ala + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Ala-7-amido-4-methylcoumarin + H2O
L-Ala + 7-amino-4-methylcoumarin
about 2% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Ala-7-amido-4-methylcoumarin + H2O
L-Ala + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-(Met)enkephalin + H2O

L-Arg + (Met)enkephalin
-
-
-
?
L-Arg-(Met)enkephalin + H2O
L-Arg + (Met)enkephalin
-
-
-
-
?
L-Arg-2-naphthylamide + H2O

L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
35982, 35986, 35991, 35998, 36000, 664535, 665109, 665836, 666534, 678547, 678924, 681632, 731369 -
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
100% activity
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
17% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-2-naphthylamide + H2O
L-Arg + 2-naphthylamine
-
-
-
-
?
L-Arg-4-nitroanilide + H2O

L-Arg + 4-nitroaniline
best substrate
-
-
?
L-Arg-4-nitroanilide + H2O
L-Arg + 4-nitroaniline
-
-
-
-
?
L-Arg-4-nitroanilide + H2O
L-Arg + 4-nitroaniline
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O

L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
100% activity
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
high activity
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
Corycaeus anglicus
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
100% activity
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
100% activity
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-7-amido-4-methylcoumarin + H2O
L-Arg + 7-amino-4-methylcoumarin
-
best substrate
-
-
?
L-Arg-p-nitroanilide + H2O

L-Arg + p-nitroaniline
-
-
-
-
?
L-Arg-p-nitroanilide + H2O
L-Arg + p-nitroaniline
-
-
-
-
?
L-Leu-2-naphthylamide + H2O

L-Leu + 2-naphthylamine
-
-
-
-
?
L-Leu-2-naphthylamide + H2O
L-Leu + 2-naphthylamine
-
31% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Leu-4-nitroanilide + H2O

L-Leu + 4-nitroaniline
-
-
-
?
L-Leu-4-nitroanilide + H2O
L-Leu + 4-nitroaniline
-
-
-
-
?
L-Leu-7-amido-4-methylcoumarin + H2O

L-Leu + 7-amino-4-methylcoumarin
28% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Leu-7-amido-4-methylcoumarin + H2O
L-Leu + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Leu-7-amido-4-methylcoumarin + H2O
L-Leu + 7-amino-4-methylcoumarin
about 1% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Leu-7-amido-4-methylcoumarin + H2O
L-Leu + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Lys-(Met)enkephalin + H2O

L-Lys + (Met)enkephalin
-
-
-
?
L-Lys-(Met)enkephalin + H2O
L-Lys + (Met)enkephalin
-
-
-
-
?
L-Lys-2-naphthylamide + H2O

L-Lys + 2-naphthylamine
-
-
-
-
?
L-Lys-2-naphthylamide + H2O
L-Lys + 2-naphthylamine
-
-
-
-
?
L-Lys-2-naphthylamide + H2O
L-Lys + 2-naphthylamine
-
100% activity
-
-
?
L-Lys-2-naphthylamide + H2O
L-Lys + 2-naphthylamine
-
41% activity compared to L-Arg-2-naphthylamide
-
-
?
L-Lys-4-nitroanilide + H2O

L-Lys + 4-nitroaniline
-
-
-
?
L-Lys-4-nitroanilide + H2O
L-Lys + 4-nitroaniline
-
-
-
-
?
L-Lys-4-nitroanilide + H2O
L-Lys + 4-nitroaniline
-
-
-
-
?
L-Lys-7-amido-4-methylcoumarin + H2O

L-Lys + 7-amino-4-methylcoumarin
10% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Lys-7-amido-4-methylcoumarin + H2O
L-Lys + 7-amino-4-methylcoumarin
about 45% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Lys-7-amido-4-methylcoumarin + H2O
L-Lys + 7-amino-4-methylcoumarin
-
17% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Met-2-naphthylamide + H2O

L-Met + 2-naphthylamine
-
-
-
-
?
L-Met-2-naphthylamide + H2O
L-Met + 2-naphthylamine
-
2% activity compared to L-Lys-2-naphthylamide
-
-
?
L-Met-7-amido-4-methylcoumarin + H2O

L-Met + 7-amino-4-methylcoumarin
19% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Met-7-amido-4-methylcoumarin + H2O
L-Met + 7-amino-4-methylcoumarin
about 1% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Met-7-amido-4-methylcoumarin + H2O
L-Met + 7-amino-4-methylcoumarin
-
no activity with Z-Met-7-amido-4-methylcoumarin
-
-
?
L-Phe-7-amido-4-methylcoumarin + H2O

L-Phe + 7-amino-4-methylcoumarin
about 5% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Phe-7-amido-4-methylcoumarin + H2O
L-Phe + 7-amino-4-methylcoumarin
-
2% activity compared to L-Arg-7-amido-4-methylcoumarin
-
-
?
L-Phe-7-amido-4-methylcoumarin + H2O
L-Phe + 7-amino-4-methylcoumarin
-
low activity
-
-
?
L-Tyr-2-naphthylamide + H2O

L-Tyr + 2-naphthylamine
-
0.171% activity compared to L-Arg-2-naphthylamide
-
-
?
L-Tyr-2-naphthylamide + H2O
L-Tyr + 2-naphthylamine
-
62% activity compared to L-Lys-2-naphthylamide
-
-
?
Leu-4-nitroanilide + H2O

Leu + 4-nitroaniline
-
-
-
?
Leu-4-nitroanilide + H2O
Leu + 4-nitroaniline
7% of the activity with Arg-4-nitroanilide
-
?
Leu-4-nitroanilide + H2O
Leu + 4-nitroaniline
7% of the activity with Arg-4-nitroanilide
-
?
Lys-2-naphthylamide + H2O

Lys + 2-naphthylamine
-
-
-
-
?
Lys-2-naphthylamide + H2O
Lys + 2-naphthylamine
-
-
-
-
?
Lys-2-naphthylamide + H2O
Lys + 2-naphthylamine
-
-
-
-
?
Lys-2-naphthylamide + H2O
Lys + 2-naphthylamine
-
-
-
-
?
Lys-4-nitroanilide + H2O

Lys + 4-nitroaniline
-
3.6% of the activity with Arg-7-amido-4-methylcoumarin
-
?
Lys-4-nitroanilide + H2O
Lys + 4-nitroaniline
5% of the activity with Arg-4-nitroanilide
-
?
additional information

?
-
substrate specificity, 4-nitroanilides of Gly, Glu, Asp, Phe, Pro, and Ala-Pro are poor substrates, overview
-
-
?
additional information
?
-
-
substrate specificity, 4-nitroanilides of Gly, Glu, Asp, Phe, Pro, and Ala-Pro are poor substrates, overview
-
-
?
additional information
?
-
-
no hydrolysis of amino acids with apolar groups, without free alpha-amino group, or anionic amino acids
-
-
?
additional information
?
-
-
the enzyme probably is involved in the final stages of peptide and protein precursor processing and maturation mechanisms via the exopeptidase pathway and thereby in some inflammatory processes and tumour development
-
-
?
additional information
?
-
-
the enzyme from testis preferably removes Arg and/or Lys residues from the N-terminus of various peptides, no activity with substrate possessing Pro at the P1 position
-
-
?
additional information
?
-
no activity with L-Ala-7-amido-4-methylcoumarin, L-Cys-7-amido-4-methylcoumarin, L-Gln-7-amido-4-methylcoumarin, L-Glu-7-amido-4-methylcoumarin, Gly-7-amido-4-methylcoumarin, L-His-7-amido-4-methylcoumarin, L-Ile-7-amido-4-methylcoumarin, L-Phe-7-amido-4-methylcoumarin, L-Pro-7-amido-4-methylcoumarin, L-Thr-7-amido-4-methylcoumarin, L-Trp-7-amido-4-methylcoumarin, L-Tyr-7-amido-4-methylcoumarin, and L-Val-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
-
no activity with L-Ala-7-amido-4-methylcoumarin, L-Cys-7-amido-4-methylcoumarin, L-Gln-7-amido-4-methylcoumarin, L-Glu-7-amido-4-methylcoumarin, Gly-7-amido-4-methylcoumarin, L-His-7-amido-4-methylcoumarin, L-Ile-7-amido-4-methylcoumarin, L-Phe-7-amido-4-methylcoumarin, L-Pro-7-amido-4-methylcoumarin, L-Thr-7-amido-4-methylcoumarin, L-Trp-7-amido-4-methylcoumarin, L-Tyr-7-amido-4-methylcoumarin, and L-Val-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
-
substrate specificity, no activity with benzoyl-Arg-2-naphthylamide, and 2-naphthylamides of Glu, Ser, and Tyr, no activity with Phe-Phe-Ala-2-naphthylamide, Leu-Gly-Gly-4-methoxy-2-naphthylamide, and Gly-Pro-Leu-2-naphthylamide, overview
-
-
?
additional information
?
-
-
substrate specificity, no activity with L-Pro-7-amido-4-methylcoumarin and L-Asp-7-amido-4-methylcoumarin, L-Ser-7-amido-4-methylcoumarin is a poor substrate, overview
-
-
?
additional information
?
-
the enzyme is induced by interferon-gamma, the enzyme can trim the N-terminal extended precursor to antigenic peptides in the endoplasmic reticulum
-
?
additional information
?
-
-
the enzyme is induced by interferon-gamma, the enzyme can trim the N-terminal extended precursor to antigenic peptides in the endoplasmic reticulum
-
?
additional information
?
-
-
the enzyme probably is involved in the final stages of peptide and protein precursor processing and maturation mechanisms via the exopeptidase pathway and thereby in some inflammatory processes and tumour development
-
-
?
additional information
?
-
-
the enzyme from testis preferably removes Arg and/or Lys residues from the N-terminus of various peptides, no activity with substrate possessing Pro at the P1 position
-
-
?
additional information
?
-
-
the enzyme is strictly specific for the removal of N-terminal basic residues from peptides and proteins
-
-
?
additional information
?
-
no activity with L-Cys-7-amido-4-methylcoumarin, L-Asp-7-amido-4-methylcoumarin, and L-Glu-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
-
no activity with L-Cys-7-amido-4-methylcoumarin, L-Asp-7-amido-4-methylcoumarin, and L-Glu-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
the aminopeptidase binding site shares a similar structure to LTA4H (EC 3.3.2.6) at its ligand binding sites
-
-
?
additional information
?
-
-
no activity with Ala-Ala, Ala-Lys, Asp-Ala, Gly-Ala and Leu-Ala. The enzyme exclusively hydrolyzes basic amino acids from the amino termini of peptide substrates. The nature of the amino acid residue at the C-terminus of the dipeptide has an effect on hydrolysis rate. The activity is maximal towards dipeptides with Arg, Lys, or Ala as the C-terminal residue
-
?
additional information
?
-
-
the enzyme probably is involved in the final stages of peptide and protein precursor processing and maturation mechanisms via the exopeptidase pathway and thereby in some inflammatory processes and tumour development
-
-
?
additional information
?
-
-
the enzyme from testis preferably removes Arg and/or Lys residues from the N-terminus of various peptides, no activity with substrate possessing Pro at the P1 position
-
-
?
additional information
?
-
-
the enzyme is strictly specific for the removal of N-terminal basic residues from peptides and proteins
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
the enzyme plays a role in peptide or protein precursor processing, the enzyme expression is up-regulated during ontogenesis
-
-
?
additional information
?
-
-
the enzyme probably is involved in the final stages of peptide and protein precursor processing and maturation mechanisms via the exopeptidase pathway and thereby in some inflammatory processes and tumour development, the enzyme from testis preferably removes Arg and/or Lys residues from the N-terminus of various peptides
-
-
?
additional information
?
-
-
the enzyme probably is involved in the final stages of peptide and protein precursor processing and maturation mechanisms via the exopeptidase pathway and thereby in some inflammatory processes and tumour development, the enzyme from testis preferably removes Arg and/or Lys residues from the N-terminus of various peptides
-
-
?
additional information
?
-
the enzyme catalyzes the N-terminal cleavage of basic residues of peptide or protein substrates
-
-
?
additional information
?
-
-
the enzyme from testis preferably removes Arg and/or Lys residues from the N-terminus of various peptides, no activity with bradykinin, neurotensin precursor and substance P, no activity with substrate possessing Pro at the P1 position
-
-
?
additional information
?
-
-
the enzyme is strictly specific for the removal of N-terminal basic residues from peptides and proteins, no activity with bradykinin, no activity with substrate possessing Pro at the P1 position
-
-
?
additional information
?
-
-
no activity with L-Ala-7-amido-4-methylcoumarin, L-Asn-7-amido-4-methylcoumarin, L-Gln-7-amido-4-methylcoumarin, L-Glu-7-amido-4-methylcoumarin, Gly-7-amido-4-methylcoumarin, L-His-7-amido-4-methylcoumarin, L-Ile-7-amido-4-methylcoumarin, L-Leu-7-amido-4-methylcoumarin, L-Asp-7-amido-4-methylcoumarin, L-Thr-7-amido-4-methylcoumarin, L-Met-7-amido-4-methylcoumarin, L-Trp-7-amido-4-methylcoumarin, L-Ser-7-amido-4-methylcoumarin, L-Tyr-7-amido-4-methylcoumarin, and L-Val-7-amido-4-methylcoumarin
-
-
?
additional information
?
-
-
no activity with L-alpha-Asn-2-naphthylamide, L-Glu-2-naphthylamide, L-Ile-2-naphthylamide, L-Phe-2-naphthylamide, L-Pro-2-naphthylamide, L-Ser-2-naphthylamide, L-Thr-2-naphthylamide, L-Trp-2-naphthylamide, L-Val-2-naphthylamide, and L-Arg-L-Arg-2-naphthylamide
-
-
?
additional information
?
-
-
no detectable activity with L-Asp-2-naphthylamide
-
-
?
additional information
?
-
proteolysis is restricted to peptides with an arginine residue in the N terminus, with cleavage detected only when a hydrophobic or an uncharged residue occupies the second site
-
?
additional information
?
-
-
proteolysis is restricted to peptides with an arginine residue in the N terminus, with cleavage detected only when a hydrophobic or an uncharged residue occupies the second site
-
?
additional information
?
-
the enzyme may serve as a critical factor for arginine acquisition during nutrient stress in vivo and also in the proteolysis of host proteins and peptides during SBE pathology
-
?
additional information
?
-
-
the enzyme may serve as a critical factor for arginine acquisition during nutrient stress in vivo and also in the proteolysis of host proteins and peptides during SBE pathology
-
?
additional information
?
-
proteolysis is restricted to peptides with an arginine residue in the N terminus, with cleavage detected only when a hydrophobic or an uncharged residue occupies the second site
-
?
additional information
?
-
-
proteolysis is restricted to peptides with an arginine residue in the N terminus, with cleavage detected only when a hydrophobic or an uncharged residue occupies the second site
-
?
additional information
?
-
the enzyme may serve as a critical factor for arginine acquisition during nutrient stress in vivo and also in the proteolysis of host proteins and peptides during SBE pathology
-
?
additional information
?
-
-
the enzyme may serve as a critical factor for arginine acquisition during nutrient stress in vivo and also in the proteolysis of host proteins and peptides during SBE pathology
-
?
additional information
?
-
-
substrate specificity, the enzyme prefers Arg or Lys in N-terminal position, no activity with dipeptide-4-nitroanilides, overview
-
-
?
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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
arphamenine
-
aminopeptidase B-specific inhibitor
-
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
-
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 actvity 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
-
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0.00006 - 0.000077
1,10-phenanthroline
0.0003
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.01
abexinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.00000316 - 0.00000402
Arphamenine A
0.0000007 - 0.00000155
Arphamenine B
0.01
belinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.00000349 - 0.0005
bestatin
0.01
CUDC-101
Homo sapiens
above, pH and temperature not specified in the publication
0.01
entinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
givinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
JNJ-26481585
Homo sapiens
above, pH and temperature not specified in the publication
0.01
mocetinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
Homo sapiens
above, pH and temperature not specified in the publication
0.01
panobinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
pracinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
resminostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
rocilinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.0044
scriptaid
Homo sapiens
pH and temperature not specified in the publication
0.00167
suberanilohydroxamic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.01
trichostatin A
Homo sapiens
above, pH and temperature not specified in the publication
0.01
tubacin
Homo sapiens
above, pH and temperature not specified in the publication
0.01
Valproate
Homo sapiens
above, pH and temperature not specified in the publication
0.00000391 - 0.00000592
ZnCl2
7.77
[(2Z)-3-[2-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
7.9
[(2Z)-3-[2-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
7.39
[(2Z)-3-[2-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
12.09
[(2Z)-3-[5-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
1.71
[(2Z)-3-[5-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
2.17
[(2Z)-3-[5-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
7.9
[(2Z)-3-[5-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
3.87
[(2Z)-3-[6-(6-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
7.19
[(2Z)-3-[6-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
6.82
[(2Z)-3-[6-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
1.3
[(2Z)-3-[6-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
12.27
[(2Z)-3-[6-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
13.53
[(2Z)-3-[6-(7-methoxy-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
10.11
[(2Z)-4-oxo-3-[2-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]ethyl]-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
14.89
[(2Z)-4-oxo-3-[5-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]pentyl]-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
7.7
[(2Z)-4-oxo-3-[6-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]hexyl]-1,3-thiazolidin-2-ylidene]cyanamide
Homo sapiens
pH 7.5, 22°C
0.00006
1,10-phenanthroline

Homo sapiens
-
pH 7.4, 37°C, mutant Q169N
0.000077
1,10-phenanthroline
Homo sapiens
-
pH 7.4, 37°C, wild-type
0.00000316
Arphamenine A

Homo sapiens
-
pH 7.4, 37°C, mutant Q169N
0.00000373
Arphamenine A
Homo sapiens
-
pH 7.4, 37°C, wild-type
0.00000402
Arphamenine A
Homo sapiens
wild type enzyme, at pH 7.4 and 37°C
0.0000007
Arphamenine B

Homo sapiens
wild type enzyme, at pH 7.4 and 37°C
0.00000072
Arphamenine B
Homo sapiens
-
pH 7.4, 37°C, wild-type
0.00000155
Arphamenine B
Homo sapiens
-
pH 7.4, 37°C, mutant Q169N
0.00000349
bestatin

Homo sapiens
-
pH 7.4, 37°C, wild-type
0.00000382
bestatin
Homo sapiens
wild type enzyme, at pH 7.4 and 37°C
0.000289
bestatin
Homo sapiens
-
pH 7.4, 37°C, mutant Q169N
0.0005
bestatin
Homo sapiens
pH 7.5, 22°C
0.00000391
ZnCl2

Homo sapiens
-
pH 7.4, 37°C, wild-type
0.00000592
ZnCl2
Homo sapiens
-
pH 7.4, 37°C, mutant Q169N
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