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3.4.21.7: plasmin

This is an abbreviated version!
For detailed information about plasmin, go to the full flat file.

Word Map on EC 3.4.21.7

Reaction

Preferential cleavage: Lys-/- > Arg-/-; higher selectivity than trypsin. Converts fibrin into soluble products =

Synonyms

actase, delta-plasmin, EC 3.4.4.14, fibrinase, fibrinolysin, More, mu-plasmin, mu-plasminogen, PL, plasmin, plasminogen, PLG, Plm, PLS, serum tryptase, thrombolysin

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.7 plasmin

Inhibitors

Inhibitors on EC 3.4.21.7 - plasmin

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(10S,13S)-10-(1H-indol-3-ylmethyl)-8,11-dioxo-N-(4-oxotetrahydrofuran-3-yl)-2-oxa-9,12-diazabicyclo[13.2.2]nonadeca-1(17),15,18-triene-13-carboxamide
-
-
(12S,15S)-12-(1H-indol-3-ylmethyl)-10,13-dioxo-N-(4-oxotetrahydrofuran-3-yl)-2-oxa-11,14-diazabicyclo[15.2.2]henicosa-1(19),17,20-triene-15-carboxamide
-
-
(4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-phenyl-propionylamino]-phenyl)-acetic acid
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.63 mM
(9S,12S)-9-(1H-indol-3-ylmethyl)-7,10-dioxo-N-(4-oxotetrahydrofuran-3-yl)-2-oxa-8,11-diazabicyclo[12.2.2]octadeca-1(16),14,17-triene-12-carboxamide
-
-
(E)-5,5'-(but-2-ene-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4Hchromen-4-one
-
about 43% residual activity at 0.4 mM
2-(3-[3-[(6-amino-hexyl)-(2-benzyloxycarbonylamino-3-phenyl-propionyl)-amino]-2-oxo-cyclohexyl]-propionylamino)-3-(1H-indol-3-yl)-propionic acid methyl ester
-
IC50: 0.024 mM
2-[(4-Aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionic acid pyridin-2-ylmethyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0042 mM
2-[3-(3-[(6-amino-hexyl)-[2-benzyloxycarbonylamino-3-(1H-indol-3-yl)-propionyl]-amino]-2-oxo-cyclohexyl)-propionylamino]-3-(1H-indol-3-yl)-propionic acid methyl ester
-
IC50: 0.02 mM
3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)heptyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one
-
about 1% residual activity at 0.4 mM
3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)octyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one
-
about 2% residual activity at 0.4 mM
4-(2-aminoethyl)benzenesulfonyl fluoride
-
-
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.024 mM, IC50 in reaction with fibrin is 0.0039 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid hexyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.018 mM, IC50 in reaction with fibrin is 0.0043 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid methyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0009 mM, IC50 in reaction with fibrin is 0.0061 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid octyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is above 0.1 mM, IC50 in reaction with fibrin is 0.005 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0014 mM, IC50 in reaction with fibrin is 0.00042 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid hexyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0015 mM, IC50 in reaction with fibrin is 0.0004 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid methyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.001 mM, IC50 in reaction with fibrin is 0.00078 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid octyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0025 mM, IC50 in reaction with fibrin is 0.00056 mM
4-amidinophenyl methane-sulfonyl fluoride
4-aminobenzamidine
-
competitive inhibition
4-aminomethylbenzamidine
-
competitive inhibition
4-carboxybenzamidine
-
competitive inhibition
479-504 peptide of factor VIII
-
blocks A2 subunit binding to Ah-plasmin by ca. 50% in a dose-dependent manner
-
484-509 peptide of factor VIII
-
blocks A2 subunit binding to Ah-plasmin by ca. 50% in a dose-dependent manner
-
489-514 peptide of factor VIII
-
weakly inhibits binding of the A2 subunit and plasmin with ca. 80% residual binding at the highest concentration (0.8 mM) of peptide
-
5,5'-(butane-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4H-chromen-4-one
-
about 42% residual activity at 0.4 mM
6-aminohexanoate
-
6-aminohexanoic acid
A2 subunit of factor VIII
-
plasmin-catalyzed activation of factor VIII is significantly inhibited by the addition of isolated A2 subunit of factor VIII in a dose-dependent manner
-
actin
-
actin inhibition of the fibrinolytic activity of plasmin is due to its competition with fibrin for the lysine binding sites of the enzyme
Aedes aegypti trypsin inhibitor
-
-
AG490
-
JAK inhibitor, inhibits JAK1 but does not inhibit TYK2 phosphorylation by plasmin. Impairs plasmin-mediated phosphorylation of ERK1/2, Akt1, and the subsequent phosphorylation of IkappaBalpha, but not that of p38 MAPK. Inhibits plasmin-induced TNF-alpha release by 63% and IL-6 release by 76%
Ah-plasmin
-
immobilized Ah-plasmin inhibits the A2 binding to Ah-plasmin by ca. 80% in a dose-dependent manner
-
AKbetaBA
-
inhibits plasmin-induced TNF-alpha release by 70%. Inhibits plasmin-induced activation of NF-kappaB by 66%
alpha(2)-plasmin inhibitor
-
alpha-antiplasmin
potent inhibitor
-
alpha-antitrypsin
-
-
-
alpha-lactalbumin
-
shows a strong correlation with plasmin activity and may have inhibitory activity against plasmin
-
alpha1 globulin
-
-
-
alpha1-protease inhibitor
-
plasmin bound to fibrin is completely protected
-
alpha2 globulin
-
-
-
alpha2-antiplasmin
-
alpha2-Macroglobulin
-
alpha2-Plasmin inhibitor
-
kringle domains K2, K3, and K5 are involved in the modulation of Plm activity
-
aminomethyl cyclohexane carboxylic acid
-
-
amyloid precursor-like protein 2
-
-
annexin II tetramer
-
promotes plasmin inactivation by stimulating the autoproteolytic digestion of plasmin heavy and light chains, also stimulates formation of plasmin. annexin II tetramer may function to provide the cell surface with a transient pulse of plasmin activity
-
antiplasmin
-
the inhibition of plasmin by antiplasmin can be reduced by high molecular weight fibrin degradation products with carboxy-terminal lysine residues
-
Aprotinin
arachidonate
-
-
arsenic acid
-
organometallic complexes composed of humic acid and arsenic acid show enhanced inhibition of plasmin activity as compared with either arsenic or humic acid alone
bdellin
-
-
benzamidine
beta-Lactoglobulin
-
native and denatured beta-lactoglobulin inhibits activity with D-Val-L-Leu-L-Lys-p-nitroanilide and casein
-
bikazin salivary inhibitor
-
-
bikunin
-
-
Blood serum
-
bovine or ovine blood serum do not affect hydrolysis of caseins in milk by plasmin. Equine and particularly porcine serum strongly inhibit casein hydrolysis. Heated serum (70°C for 5 min) from any of the species does not influence plasmin-induced hydrolysis of caseins. Bovine or ovine serum (2%) have no effect on plasmin activity when assayed on N-Suc-L-Ala-L-Phe-L-Lys-7-amido-4-methyl-coumarin in milk. 2.0% porcine serum reduces plasmin activity on this peptide by ca. 40%
-
C1 inhibitor
-
the C1-inhibitor in its native state inhibits plasmin without significant degradation. If the C1-inhibitor is in a denatured polymeric state as can easily occur during storage, or as produced by heating of the native protein, it will be extensively degraded by plasmin
-
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0062 mM, IC50 in reaction with fibrin is 0.0012 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-heptylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.011 mM, IC50 in reaction with fibrin is 0.0033 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-hexylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.013 mM, IC50 in reaction with fibrin is 0.0027 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-nonylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0083 mM, IC50 in reaction with fibrin is 0.0013 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-octylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.007 mM, IC50 in reaction with fibrin is 0.0018 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-pentylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.01 mM, IC50 in reaction with fibrin is 0.0013 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.085 mM, IC50 in reaction with fibrin is 0.019 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-butyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.009 mM, IC50 in reaction with fibrin is 0.0023 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-hexyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.006 mM, IC50 in reaction with fibrin is 0.0035 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-pentyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.009 mM, IC50 in reaction with fibrin is 0.0047 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-propylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0092 mM, IC50 in reaction with fibrin is 0.002 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.013 mM, IC50 in reaction with fibrin is 0.0017 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(3-methyl-butylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00046 mM, IC50 in reaction with fibrin is 0.000056 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-butyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00079 mM, IC50 in reaction with fibrin is 0.00009 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-ethyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00063 mM, IC50 in reaction with fibrin is 0.000098 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-hexyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00049 mM, IC50 in reaction with fibrin is 0.00024 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-methoxymethyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00023 mM, IC50 in reaction with fibrin is mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-pentyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00057 mM, IC50 in reaction with fibrin is 0.00007 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(pyridin-4-ylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00098 mM, IC50 in reaction with fibrin is 0.00017 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-heptylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.00043 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-hexylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0012 mM, IC50 in reaction with fibrin is 0.00038 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-nonylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
potent and selective inhibitor for plasmin, IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0005 mM, IC50 in reaction with fibrin is 0.0001 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-pentylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.011 mM, IC50 in reaction with fibrin is 0.0001 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[(pyridin-2-ylmethyl)-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0015 mM, IC50 in reaction with fibrin is 0.00052 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[(pyridin-4-ylmethyl)-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is0.0053 mM, IC50 in reaction with fibrin is 0.0014 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[benzyl-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.0003 mM
chicken liver trypsin inhibitor
-
-
Cholesterol sulfate
-
reduces plasmin activity in a dose-dependent manner
cis-parinaric acid
-
more than 60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
CO
-
CO elicits hypofibrinolysis by enhancing alpha2-antiplasmin activity and decreasing plasmin activity
CU-2010
potent inhibitpr
-
D-Ile-Phe-Lys
-
D-Ile-Phe-Lys-CH2Cl
-
D-Ile-Phe-Lys-CN
-
-
D-Ile-Phe-Lys-NH2
-
-
D-Leu-Lys-benzylamide
-
weak inhibitor of amidolytic activity
D-Phe-Lys-benzylamide
-
inhibition of fibrinolytic activity, no inhibition of amidolytic activity
D-Val-Phe-Lys-chloromethyl ketone
-
inhibits the ability of plasmin to potentiate lipopolysaccharide signalling. Significantly inhibits the generation of TNFalpha from untransfected RAW cells after plasmin pretreatment and stimulated with LPS
diisopropyl fluorophosphate
-
does not block binding of hepatocytes from mice to immobilized plasmin, but blocks active site of plasmin and its ability to phosphorylate ERK1/2
discreplasminin
-
isolated from Tityus discrepans scorpion venom. Peptide with a relative molecular weight of less than 6000 Da and a pI value of 8.0. Discreplasminin strongly inhibits plasmin and moderately inhibits tissue plasminogen activator
-
disodium 2-methoxy-4-[(1E)-3-[4-methyl-2-(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 73% residual activity at 0.4 mM
disodium 2-methoxy-6-[(1E)-3-oxo-3-[2-(sulfonatooxy)phenyl]prop-1-en-1-yl]phenyl sulfate
-
about 40% residual activity at 0.4 mM
disodium 3,5-dimethoxy-2-[(2E)-3-[3-methoxy-4-(sulfonatooxy)phenyl]prop-2-enoyl]phenyl sulfate
-
about 40% residual activity at 0.4 mM
disodium 3,5-dimethoxy-2-[(2E)-3-[4-methoxy-3-(sulfonatooxy)phenyl]prop-2-enoyl]phenyl sulfate
-
about 75% residual activity at 0.4 mM
disodium 3-(4-oxo-3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 40% residual activity at 0.4 mM
disodium 3-(acetyloxy)-5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 84% residual activity at 0.4 mM
disodium 3-[4-oxo-3-[3-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]propyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 35% residual activity at 0.4 mM
disodium 4-(4-oxo-3,4-dihydroquinazolin-2-yl)benzene-1,3-diyl disulfate
-
about 77% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[5-[5-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]pentyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 25% residual activity at 0.4 mM; about 35% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 5% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[[1-(12-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]dodecyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 2% residual activity at 0.4 mM; about 30% residual activity at 0.4 mM; about 40% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[[1-(7-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]heptyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 30% residual activity at 0.4 mM
disodium 4-[(2E)-3-(2-methoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate
-
about 39% residual activity at 0.4 mM
disodium 4-[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate
-
about 31% residual activity at 0.4 mM
disodium 4-[4-oxo-3-[11-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]undecyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 3% residual activity at 0.4 mM
disodium 4-[4-oxo-3-[8-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]octyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 7% residual activity at 0.4 mM
disodium 4-[4-oxo-3-[9-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]nonyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 7% residual activity at 0.4 mM
disodium 4-[4-oxo-6-(sulfonatooxy)-4H-chromen-2-yl]phenyl sulfate
-
about 85% residual activity at 0.4 mM
DX-1000
-
-
elaidic acid
-
60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
epsilon-aminocaproic acid
-
inhibits plasmin-induced phosphorylation of ERK1/2; lysine binding sites inhibitor, partially blocks binding of hepatocytes from mice to immobilized plasmin at 10 mM, but not at 0.01 mM
Fibrin
-
inhibits hydrolysis of D-Val-Leu-Lys-p-nitroanilide
fibrinogen
-
fragment X
-
competitive inhibitor of plasmin chromogenic activity
-
histidine-rich glycoprotein
binds at sites of tissue injury and seems to act as a high-affinity receptor to immobilize plasminogen on cell surfaces
-
human aprotinin analogue
-
-
-
human plasma protein inhibitors
-
-
-
humic acid
-
0.02-0.48 mg/ml, up to 95% inhibition, natural and synthetic. Organometallic complexes composed of humic acid and arsenic acid show enhanced inhibition of plasmin activity as compared with either arsenic or humic acid alone
hydroxyethyl starch 130
-
plasma diluted with hydroxyethyl starch 130 has a significant more than 25% attenuation of plasmin-mediated decreases in the maximum rate of thrombus generation and total thrombus generation compared with 0.9% NaCl diluted and undiluted plasma. Enhances fibrinolysis by diminishing alpha2-antiplasmin-plasmin interactions
-
infestin
-
-
KD1-L17R
-
-
KM(O2)YR-H
-
Kunitz-type inhibitor 2
-
-
L-Ile-Phe-Lys
-
L-lysine
-
-
L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
LEKTI
-
potent noncompetitive inhibitor, recombinant LEKTI is purified using a baculovirus/insect cell expression system
Leu-Lys-benzylamide
-
inhibition of fibrinolytic activity, no inhibition of amidolytic activity
Leucaena-type trypsin inhibitor
-
-
leupeptin
-
inhibits the ability of plasmin to potentiate lipopolysaccharide signalling
Lima bean trypsin inhibitor
-
-
-
Lys-Met(sulfone)-Tyr-Arg
-
shows 25fold selectivity for plasmin over plasma kallikrein
mAb413
-
antibody of A2 subunit, that blocks plasmin-catalyzed factor VIII heavy chain cleavage at Arg336 and Arg372, but not at Arg740. This antibody does not affect plasmin-catalyzed cleavage of the light chain
-
MG-132
-
prevents facilitation of degradation of Bim(EL) by plasmin in hepatocytes from mice pretreated with cycloheximide
MgCl2
-
0.01 M and above
N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzyloxycarbonyl)-octylamide
-
potent and selective inhibitor for plasmin, IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00023 mM, IC50 in reaction with fibrin is 0.0008 mM
N-oleoyl heparin
-
noncompetitive inhibition
-
N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-(pyridin-4-ylmethoxy)benzamide
-
molecular modeling
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-1-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-2-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-3-[[(4-fluorophenyl)acetyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-3-[[3-(1H-indol-3-yl)propanoyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1-glycyl-4-oxopyrrolidin-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclohexyl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclopentyl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobenzyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobutyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-tryptophanamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(5-aminopentyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(7-aminoheptyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-[(trans-4-aminocyclohexyl)methyl]-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
Nalpha-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-N-hexyl-O-(pyridin-4-ylmethyl)-L-tyrosinamide
-
binding mode
natural aprotinin
-
-
-
neuroserpin
-
nexin 2
-
-
Nomega-nitro-L-arginine methyl ester
-
almost completely abolishes plasmin-induced relaxation
octasodium [(ethane-1,2-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-4,1,2-triyl] tetrasulfate
-
about 16% residual activity at 0.4 mM; about 18% residual activity at 0.4 mM; about 65% residual activity at 0.4 mM
octasodium [(propane-1,3-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-1,2,4-triyl] tetrasulfate
-
about 30% residual activity at 0.4 mM
oleic acid
-
59% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
ONO-3307
i.e. 4-sulfamoyl phenyl-4-guanidinobenzoate methanesulfonate
Pancreatic trypsin inhibitor
-
PD98059
-
MEK inhibitor, completely abolishes plasmin-induced phosphorylation of ERK1/2 at 0.05 mM
pefabloc
-
-
Pentamidine
-
competitive inhibition
pentasodium (2R)-2-[3,4-bis(sulfonatooxy)phenyl]-3,4-dihydro-2H-1-benzopyran-3,6,7-triyl trisulfate
-
about 32% residual activity at 0.4 mM
pentasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-5-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methoxy]-4H-1-benzopyran-3,7-diyl disulfate
-
about 5% residual activity at 0.4 mM
pentasodium 2-[3-[2,5-bis(sulfonatooxy)phenyl]propanoyl]-5,8-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 73% residual activity at 0.4 mM
pentasodium 2-[3-[2,5-bis(sulfonatooxy)phenyl]propanoyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 60% residual activity at 0.4 mM
pentasodium 2-[4-[2,5-bis(sulfonatooxy)phenyl]butanoyl]-5,8-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 78% residual activity at 0.4 mM
pentasodium 2-[4-[2,5-bis(sulfonatooxy)phenyl]butanoyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 80% residual activity at 0.4 mM
pentasodium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 75% residual activity at 0.4 mM
pentasopentasodium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylatedium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 70% residual activity at 0.4 mM
peptide GHRPYam
-
delays appearance of plasmin activity
peroxynitrite
-
50% inhibition at 280 microM and an enzyme concentration of 10 microM
Phe-Lys-benzylamide
-
inhibition of fibrinolytic activity, no inhibition of amidolytic activity
plasminogen activator inhibitor 1
-
-
plasminogen activator inhibitor I
-
plasminogen activator inhibitor II
-
plasminogen activator inhibitor-type 1
-
totally blocks plasmin activity and degradation of casein
-
plasminogen activator inhibitors 1
-
-
plasminogen activator inhibitors 2
-
-
plasminostreptin
-
-
Protein C inhibitor
-
from Bos taurus
-
PSI-112
-
-
R484A mutant of A2
-
subunit of factor VIII, possessing ca. 250fold reduced affinity for plasmin, weakly inhibits factor VIIIa inactivation by ca. 20%
-
recombinant aprotinin
-
-
-
RG1192
-
dextran containing carboxymethylsulfate as well as benzylamide groups. Lysine-binding site domain of plasmin is the RG1192 binding site. In addition RG1192 blocks the generation of plasmin from Glu-plasminogen and inhibits the plasmin-mediated proteolysis of fibronectin and laminin
-
RG1503
-
-
-
SB203580
-
inhibits plasmin-induced TNF-alpha release by 75% and IL-6 release by 79%
serpinb2
-
steroid-treated ovariectomized mice deficient in tissue inhibitor of metalloprotease-1 and exposed to estrogen show a significant increase in plasmin activity. Increase is probably due to reduced expression of plasmin inhibitors serpinb7 and serpinb2
-
serpinb7
-
steroid-treated ovariectomized mice deficient in tissue inhibitor of metalloprotease-1 and exposed to estrogen show a significant increase in plasmin activity. Increase is probably due to reduced expression of plasmin inhibitors serpinb7 and serpinb2. Serpinb7 is localized to luminal and glandular epithelial cells of the uterus. Expression of serpinb7 is decreased by estrogen and shows an inverse relationship with plasmin activity
-
sodium 2,6-diformyl-4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 93% residual activity at 0.4 mM
sodium 3-(3-[[1-(4-[2-[3-(acetyloxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 55% residual activity at 0.4 mM
Soybean trypsin inhibitor
-
streptokinase
-
-
-
sucrose octasulfate
-
about 99% residual activity at 0.4 mM
sulfated polyvinylalcohol-acrylate copolymers
-
both the amidolytic and fibrinolytic activities are inhibited
-
TdPI tryptase inhibitor
-
-
tert-butyl 3-(3-[[5-[[(1S)-5-amino-1-cyanopentyl]carbamoyl]-2-(pyridin-4-ylmethoxy)phenyl]amino]-3-oxopropyl)-1H-indole-1-carboxylate
-
-
tetrasodium 2-[2,4-bis(sulfonatooxy)phenyl]-5-hydroxy-4-oxo-4H-chromene-3,7-diyl disulfate
-
about 45% residual activity at 0.4 mM
tetrasodium 2-[2-[6,7-bis(sulfonatooxy)-3,4-dihydroisoquinolin-2(1H)-yl]-2-oxoethyl]-1,4-phenylene disulfate
-
about 60% residual activity at 0.4 mM
tetrasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-4H-chromene-3,7-diyl disulfate
-
about 99% residual activity at 0.4 mM
tetrasodium 2-[4-[5,6-bis(sulfonatooxy)-3,4-dihydroisoquinolin-2(1H)-yl]-4-oxobutyl]-1,4-phenylene disulfate
-
about 48% residual activity at 0.4 mM
tetrasodium 4-[5-hydroxy-4-oxo-3,7-bis(sulfonatooxy)-4H-chromen-2-yl]benzene-1,2-diyl disulfate
-
about 93% residual activity at 0.4 mM
tetrasodium 5-methoxy-2-[3-[[1-(4-[2-[3-methoxy-4-(sulfonatooxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4-oxo-4H-1-benzopyran-3,7-diyl disulfate
-
about 3% residual activity at 0.4 mM; about 7% residual activity at 0.4 mM; about 8% residual activity at 0.4 mM
tetrasodium 5-methoxy-4-oxo-2-[3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4H-1-benzopyran-3,7-diyl disulfate
-
about 20% residual activity at 0.4 mM
textilinin-1
-
tissue factor pathway inhibitor-1
-
-
tissue factor pathway inhibitor-2
-
-
Tra-Tyr(O-Pic)-CONH-(C6H6)-(CH2)4-CH3
-
Tra-Tyr(O-Pic)-CONH-(C6H6)-CH2-CH3
-
Tra-Tyr(O-Pic)-CONH-(CH2)2-CH(CH3)-CH3
-
Tra-Tyr(O-Pic)-CONH-(CH2)7-COOH
-
Tra-Tyr(O-Pic)-CONH-(CH2)7-NH2
-
Tranexamic acid
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
-
-
trans-parinaric acid
-
60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
transforming growth factor-b1
-
reduces plasminogen conversion to active plasmin in wild type tendon cells
-
trisodium 2-[(1E)-3-[2,4-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 42% residual activity at 0.4 mM
trisodium 4-oxo-2-[3-(sulfonatooxy)phenyl]-4H-chromene-3,7-diyl disulfate
-
about 82% residual activity at 0.4 mM
trisodium 4-[(1E)-3-[2,4-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 58% residual activity at 0.4 mM
trisodium 4-[(1E)-3-[2,5-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]-2-methoxyphenyl sulfate
-
about 90% residual activity at 0.4 mM
trisodium 4-[(1E)-3-[2,5-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 51% residual activity at 0.4 mM
trisodium 5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)-1,3-phenylene disulfate
-
about 45% residual activity at 0.4 mM
VFK-CMK
-
-
YO-2
i.e. Tra-Tyr(O-Pic)-CONH-(CH2)7-CH3
[4-[(N-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-L-phenylalanyl)amino]phenyl]acetic acid
-
binding mode
additional information
-