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
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3.4.21.7
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fibrinolysis
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fibrinogen
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urokinase
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coagulation
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clot
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tissue-type
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thrombin
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pai-1
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endothelial
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urokinase-type
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artery
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platelet
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upa
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thrombosis
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thrombolytic
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antithrombin
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streptokinase
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heparin
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inhibitor-1
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bleeding
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infarct
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kringle
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prothrombin
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coronary
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venous
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hemorrhage
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d-dimers
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kallikrein
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anticoagulant
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stroke
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hemostatic
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zymogen
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thromboembolic
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zymography
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intravascular
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thromboplastin
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aprotinin
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2-macroglobulin
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amidolytic
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thrombin-antithrombin
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hypercoagulable
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tranexamic
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lipoproteina
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procoagulant
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antifibrinolytic
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recanalization
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prekallikrein
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alteplase
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fibrinopeptide
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nutrition
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analysis
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medicine
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degradation
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pharmacology
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thrombophilia
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agriculture
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food industry
- 3.4.21.7
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fibrinolysis
- fibrinogen
- urokinase
- coagulation
- clot
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tissue-type
- thrombin
- pai-1
- endothelial
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urokinase-type
- artery
- platelet
- upa
- thrombosis
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thrombolytic
- antithrombin
- streptokinase
- heparin
- inhibitor-1
- bleeding
- infarct
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kringle
- prothrombin
- coronary
- venous
- hemorrhage
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d-dimers
- kallikrein
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anticoagulant
- stroke
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hemostatic
- zymogen
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thromboembolic
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zymography
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intravascular
- thromboplastin
- aprotinin
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2-macroglobulin
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amidolytic
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thrombin-antithrombin
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hypercoagulable
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tranexamic
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lipoproteina
-
procoagulant
-
antifibrinolytic
-
recanalization
- prekallikrein
- alteplase
-
fibrinopeptide
- nutrition
- analysis
- medicine
- degradation
- pharmacology
- thrombophilia
- agriculture
- food industry
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
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Inhibitors
Inhibitors on EC 3.4.21.7 - plasmin
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(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
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(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
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(4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-phenyl-propionylamino]-phenyl)-acetic acid
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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
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(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
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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
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IC50: 0.024 mM
2-[(4-Aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionic acid pyridin-2-ylmethyl ester
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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
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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
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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
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about 2% residual activity at 0.4 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
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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
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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
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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
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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
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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
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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
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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
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IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0025 mM, IC50 in reaction with fibrin is 0.00056 mM
479-504 peptide of factor VIII
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blocks A2 subunit binding to Ah-plasmin by ca. 50% in a dose-dependent manner
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484-509 peptide of factor VIII
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blocks A2 subunit binding to Ah-plasmin by ca. 50% in a dose-dependent manner
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489-514 peptide of factor VIII
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weakly inhibits binding of the A2 subunit and plasmin with ca. 80% residual binding at the highest concentration (0.8 mM) of peptide
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5,5'-(butane-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4H-chromen-4-one
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about 42% residual activity at 0.4 mM
A2 subunit of factor VIII
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plasmin-catalyzed activation of factor VIII is significantly inhibited by the addition of isolated A2 subunit of factor VIII in a dose-dependent manner
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actin
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actin inhibition of the fibrinolytic activity of plasmin is due to its competition with fibrin for the lysine binding sites of the enzyme
AG490
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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
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immobilized Ah-plasmin inhibits the A2 binding to Ah-plasmin by ca. 80% in a dose-dependent manner
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AKbetaBA
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inhibits plasmin-induced TNF-alpha release by 70%. Inhibits plasmin-induced activation of NF-kappaB by 66%
alpha-lactalbumin
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shows a strong correlation with plasmin activity and may have inhibitory activity against plasmin
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alpha2-Plasmin inhibitor
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kringle domains K2, K3, and K5 are involved in the modulation of Plm activity
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annexin II tetramer
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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
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antiplasmin
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the inhibition of plasmin by antiplasmin can be reduced by high molecular weight fibrin degradation products with carboxy-terminal lysine residues
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arsenic acid
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organometallic complexes composed of humic acid and arsenic acid show enhanced inhibition of plasmin activity as compared with either arsenic or humic acid alone
beta-Lactoglobulin
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native and denatured beta-lactoglobulin inhibits activity with D-Val-L-Leu-L-Lys-p-nitroanilide and casein
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Blood serum
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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%
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C1 inhibitor
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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
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Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.0003 mM
cis-parinaric acid
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more than 60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
CO
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CO elicits hypofibrinolysis by enhancing alpha2-antiplasmin activity and decreasing plasmin activity
D-Phe-Lys-benzylamide
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inhibition of fibrinolytic activity, no inhibition of amidolytic activity
D-Val-Phe-Lys-chloromethyl ketone
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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
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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
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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
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disodium 2-methoxy-4-[(1E)-3-[4-methyl-2-(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
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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
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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
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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
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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
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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
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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
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about 35% residual activity at 0.4 mM
disodium 4-(4-oxo-3,4-dihydroquinazolin-2-yl)benzene-1,3-diyl disulfate
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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
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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
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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
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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
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about 30% residual activity at 0.4 mM
disodium 4-[(2E)-3-(2-methoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate
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about 39% residual activity at 0.4 mM
disodium 4-[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate
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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
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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
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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
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about 7% residual activity at 0.4 mM
disodium 4-[4-oxo-6-(sulfonatooxy)-4H-chromen-2-yl]phenyl sulfate
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about 85% residual activity at 0.4 mM
elaidic acid
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60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
epsilon-aminocaproic acid
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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
histidine-rich glycoprotein
binds at sites of tissue injury and seems to act as a high-affinity receptor to immobilize plasminogen on cell surfaces
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humic acid
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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
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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
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LEKTI
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potent noncompetitive inhibitor, recombinant LEKTI is purified using a baculovirus/insect cell expression system
Leu-Lys-benzylamide
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inhibition of fibrinolytic activity, no inhibition of amidolytic activity
leupeptin
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inhibits the ability of plasmin to potentiate lipopolysaccharide signalling
Lys-Met(sulfone)-Tyr-Arg
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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
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-[(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-[(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
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
PD98059
-
MEK inhibitor, completely abolishes plasmin-induced phosphorylation of ERK1/2 at 0.05 mM
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
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-type 1
-
totally blocks plasmin activity and degradation of casein
-
R484A mutant of A2
-
subunit of factor VIII, possessing ca. 250fold reduced affinity for plasmin, weakly inhibits factor VIIIa inactivation by ca. 20%
-
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
-
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
sulfated polyvinylalcohol-acrylate copolymers
-
both the amidolytic and fibrinolytic activities are inhibited
-
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
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
[4-[(N-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-L-phenylalanyl)amino]phenyl]acetic acid
-
binding mode
-
abolishes plasmin-induced Ca2+ elevation by its pretreatment of plasmin
4-amidinophenyl methane-sulfonyl fluoride
-
substantially abrogates the relaxing effect of plasmin. Abolishes plasmin-induced Ca2+ elevation by its pretreatment of plasmin
-
blocks the interactions between light chain and plasmin in a dose-dependent manner by more than 90%. Blocks A2 subunit and plasmin interaction weakly by ca. 30%. Inhibitory effect of 6-aminohexanoic acid on the interaction between the heavy chain or factor VIII and Ah-plasmin is similar to that for the A2 interaction
6-aminohexanoic acid
-
the heavy chain plays an important role in the inhibition of the enzyme by 6-aminohexanoate
-
kinetics of plasmin type 1 and 2 inhibition in absence of soluble fibrin or epsilon-caproic acid is a reversible slow binding inhibition with an initial loose complex and a following tight complex. Epsilon-amino-caproic acid slows down the first step of the reaction without effect on the second step. Fibrin slows down both reaction steps
-
alpha2-antiplasmin
-
inhibitory activity is neutralized by addition of the antibody against alpha2-antiplasmin
-
alpha2-antiplasmin
-
similar inhibition of native enzyme and deletion mutant lacking the middle portion of the molecule
-
alpha2-antiplasmin
-
inactivation is reduced in plasmin that is bound to fibrin
-
alpha2-antiplasmin
-
plasmin inhibitor, completely blocks ability of noninhibitory plasminogen activator inhibitor-type 1 to normalize ECM degradation
-
-
similar inhibition 0f native enzyme and deletion mutant lacking the middle portion of the molecule
-
-
complete inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
Aprotinin
-
in a mouse tail-vein bleeding model, intravenous textilinin-1 and aprotinin cause similar decreases in blood loss while time to hemostasis in the textilinin-treated animals is significantly shorter
Aprotinin
-
plasmin inhibitor, completely blocks ability of noninhibitory plasminogen activator inhibitor-type 1 to normalize ECM degradation
fibrinogen
-
inhibits hydrolysis of D-Val-Leu-Lys-p-nitroanilide. 6-aminohexanoic acid abolishes inhibition
-
mainly expressed in the brain, a serpin and single-chain glycoprotein of 55 kDa containing three potential N-glycosylation sites at Asn141, Asn305, and Asn385
-
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
plasminogen activator inhibitor I
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
plasminogen activator inhibitor II
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
-
textilinin-1 is a Kunitz-type serine protease inhibitor isolated from the venom of the Australian common brown snake, Pseudonaja textilis. This molecule binds to and blocks the activity plasmin
-
textilinin-1
-
potent and reversible inhibition. At 5 microM almost complete inhibition of tissue plasminogen activator-induced fibrinolysis of whole blood clots without affecting the activated partial thromboplastin time for plasma. In a mouse tail-vein bleeding model, intravenous textilinin-1 and aprotinin cause similar decreases in blood loss while time to hemostasis in the textilinin-treated animals is significantly shorter
-
-
a synthetic inhibitor efficiently decreasing plasmin activity, plasmin inhibition by tranexamic acid upregulates the profibrogenic genes, which respond to TGF-beta-intracellular signalling
Tranexamic acid
-
plasmin inhibitor, completely blocks ability of noninhibitory plasminogen activator inhibitor-type 1 to normalize ECM degradation
-
thermosonication at an average power of 115 W for 3 min decreases the total plasmin activity by nearly 94% in fresh skim milk and cream
-
additional information
-
inhibition of ERK1/2 by MEK inhibitor U0126 does not affect plasmin-mediated expression of TNF-alpha
-
additional information
-
synthetic peptides GHRPam, GHRPLam, and GHRPYam mimicking the B knobs, render fibrin less vulnerable to attack by plasmin. None of the three synthetic peptides have a significant effect on the plasmin catalyzed hydrolysis of the chromogenic peptide D-Val-Leu-Lys-p-nitroanilide. Even in the absence of synthetic peptides there is a lag in plasmin generation accompanying fibrin formation
-
additional information
-
dilution of normal plasma with 0.9% NaCl does not significantly affect plasmin-mediated decreases in the maximum rate of thrombus and total thrombus generation compared with undiluted plasma
-
additional information
-
inactive plasmin, in which the catalytic site has been irreversibly blocked with a peptide inhibitor
-
additional information
-
development and evaluation of alternative potent and selective serine lysine analogues to inhibit plasmin, usage of a noncombinatorial peptide library to define plasmin's extended substrate specificity and guide the design of potent transition state analogue inhibitors, molecular modeling, overview
-
additional information
-
preparation and analysis of lysine-nitrile derivatives having a trisubstituted benzene for inhibitory activities against plasmin and the highly homologous plasma kallikrein and urokinase. Development of specific and selective inhibitors based on 9, overview. No inhibition by N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-methoxybenzamide
-
additional information
features and mode of action of plasmin inhibitors, detailed overview
-
additional information
-
L-methionine and L-alanine show minimal reductions of enzyme activity, even at 125 mM
-
additional information
-
noninhibitory plasminogen activator inhibitor-type 1 has no effect on plasmin activity and degradation of casein
-
additional information
-
pretreatment with plasmin, thrombin and trypsin significantly but, only partly, attenuates subsequent relaxation induced by plasmin. Major part of the plasmin-induced relaxation is resistant to these pretreatments
-
additional information
-
peptide inhibitors that incorporate 3-oxotetrahydrofuran and 3-oxotetrahydrothiophene 1,1-dioxide groups have the highest activities. For cyclopentanone-based inhibitors, incorporation of electron-withdrawing groups such as O and SO2 into the ring improves their activities. Alkylamino substituents, with an optimal spacer length of 6 carbon atoms, can be added to the inhibitors to bind in the S1 subsite. Incorporating conformationally constrained peptide segments into the inhibitors do not improve their activities
-