Information on EC 3.4.21.7 - plasmin

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The expected taxonomic range for this enzyme is: Eutheria

EC NUMBER
COMMENTARY hide
3.4.21.7
-
RECOMMENDED NAME
GeneOntology No.
plasmin
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Preferential cleavage: Lys-/- > Arg-/-; higher selectivity than trypsin. Converts fibrin into soluble products
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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endopeptidase
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CAS REGISTRY NUMBER
COMMENTARY hide
9001-90-5
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Mus musculus C57BL/6
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
synthetic construct
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
besides the main physiological inhibitor alpha2-antiplasmin, the plasmin-antiplasmin system is also regulated by the general protease inhibitor alpha2-macroglobulin, a member of the protease inhibitor I39 family. The activity of the plasminogen activators is primarily regulated by the plasminogen activator inhibitors 1 and 2, members of the serine protease inhibitor superfamily
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
Ac-FM(O2)YK-4-nitroanilide + H2O
Ac-FM(O2)YK + 4-nitroaniline
show the reaction diagram
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
Ac-KM(O2)FR-4-nitroanilide + H2O
Ac-KM(O2)FR + 4-nitroaniline
show the reaction diagram
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
Ac-KM(O2)YR + H2O
?
show the reaction diagram
-
-
-
?
Ac-KM(O2)YR-4-nitroanilide + H2O
Ac-KM(O2)YR + 4-nitroaniline
show the reaction diagram
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
Ac-RM(O2)WR-4-nitroanilide + H2O
Ac-RM(O2)WR + 4-nitroaniline
show the reaction diagram
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
Ac-RM(O2)YR + H2O
?
show the reaction diagram
-
-
-
?
Ac-RM(O2)YR-4-nitroanilide + H2O
Ac-RM(O2)YR + 4-nitroaniline
show the reaction diagram
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
ADAMTS13 + H2O
?
show the reaction diagram
AIYRSR + H2O
AIYR + Ser-Arg
show the reaction diagram
-
-
-
?
alpha-lactalbumin + H2O
?
show the reaction diagram
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
alphaS-casein + H2O
?
show the reaction diagram
-
hydrolysis is highly dependent on photooxidation state of substrate
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-
?
alphas1-casein + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid beta peptide Abeta42 + H2O
?
show the reaction diagram
-
cleavage prevents the aggregation of Abeta42 and its cleavage products into beta-pleated sheet structure
-
?
amyloid-beta + H2O
?
show the reaction diagram
annexin A2 + H2O
?
show the reaction diagram
benzyloxycarbonyl-Lys-p-nitrophenyl ester + H2O
?
show the reaction diagram
-
-
-
-
?
beta-casein + H2O
?
show the reaction diagram
beta-lactoglobulin + H2O
?
show the reaction diagram
-
hydrolysis is highly dependent on photooxidation state of substrate
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?
beta2-glycoprotein I + H2O
?
show the reaction diagram
-
in human plasma beta2-glycoprotein I is proteolytically cleaved by plasmin in its domain V (nicked beta2GPI), resulting in binding to plasminogen
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-
?
Boc-Glu-Lys-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Glu-Lys-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Boc-Val-Leu-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
C1 inhibitor + H2O
?
show the reaction diagram
-
the C1-inhibitor in its native state inhibits plasmin without significant degradation. If the C1-inhibtor 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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?
cadherin + H2O
?
show the reaction diagram
-
plasmin bound to pneumococci is able to cleave recombinant vascular endothelial cadherin
-
-
?
carboxypeptidase N + H2O
?
show the reaction diagram
-
plasmin cleaves the 83 kDa subunit of carboxypeptidase N between Arg457 and Ser458 and after prolonged incubation between Arg218 and Arg219. The small 55 kDa is cleaved to a 48 kDa product. The cleavage enhances the activity of carboxypeptidase N to 150% of the uncleaved enzyme
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-
?
casein + H2O
?
show the reaction diagram
chromogenic substrate S-2551 + H2O
?
show the reaction diagram
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-
-
?
chromogranin A + H2O
catestatin + ?
show the reaction diagram
-
chromogranin A-wild-type, chromogranin A-Gly364Ser and chromogranin A-Arg374Gln completely digested with plasmin at 0.0004 mM
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?
chromogranin A + H2O
hCgA-(360-373) + ?
show the reaction diagram
chromozyme PL + H2O
?
show the reaction diagram
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?
CIYRSR + H2O
CIYR + Ser-Arg
show the reaction diagram
-
-
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?
complement component C3 + H2O
complement component C3a + ?
show the reaction diagram
-
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?
complement component C3a + H2O
?
show the reaction diagram
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?
complement component C3b + H2O
?
show the reaction diagram
-
the enzyme inactivates the C3b molecule for complement C3b amplification
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?
D-Ile-Phe-Lys + H2O
?
show the reaction diagram
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-
-
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?
D-Nle-hexa-hydrotyrosyl-Lys-4-nitroanilide + H2O
D-Nle-hexa-hydrotyrosyl-Lys + 4-nitroaniline
show the reaction diagram
-
-
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?
D-Nle-hexahydrotyrosyl-Lys-4-nitroanilide + H2O
D-Nle-hexahydrotyrosyl-Lys + 4-nitroanilide
show the reaction diagram
-
-
-
?
D-norleucyl-hexahydrotyrosyl-lysine-p-nitroanilide + H2O
?
show the reaction diagram
synthetic construct
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-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
show the reaction diagram
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroanilide
show the reaction diagram
-
-
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?
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
show the reaction diagram
D-Val-Leu-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
show the reaction diagram
D-valyl-L-leucyl-L-lysine-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
epithelial sodium channel + H2O
epithelial sodium channel gamma subunit + ?
show the reaction diagram
-
-
-
-
?
epithelial sodium channel gamma subunit + H2O
?
show the reaction diagram
-
plasmin activates epithelial sodium channels in association with inducing cleavage of the gamma subunit at gammaLys194, a site distal to the furin site. A gammaK194A mutant epithelial sodium channel subunit prevents both plasmin-dependent activation of epithelial sodium channel and plasmin-dependent production of a unique 70-kDa carboxyl-terminal gamma subunit cleavage fragment
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?
ERK1/2
?
show the reaction diagram
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triggers activation
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?
factor VIII + H2O
?
show the reaction diagram
Fibrin + H2O
?
show the reaction diagram
fibrin + H2O
soluble fibrin fragments
show the reaction diagram
Fibrinogen + H2O
?
show the reaction diagram
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?
fibrinogen + H2O
fragment X
show the reaction diagram
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fragment X generated by limited plasmin digestion of fibrinogen
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?
Fibronectin + H2O
?
show the reaction diagram
-
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-
-
?
GIVRSR + H2O
GIVR + Ser-Arg
show the reaction diagram
-
-
-
?
GIYRSR + H2O
GIYR + Ser-Arg
show the reaction diagram
-
-
-
?
Glu-plasminogen + H2O
angiostatin 4.5 (AS4.5)
show the reaction diagram
-
AS4.5 is prepared from Glu-plasminogen by plasmin digestion
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-
?
GPGRVV + H2O
GPGR + Val-Val
show the reaction diagram
-
-
-
?
H-D-norleucyl-hexahydrotyrosol-lysine-para nitroanilide diacetate + H2O
?
show the reaction diagram
-
-
-
-
?
H-D-Val-Leu-Lys-p-nitroaniline dihydrochloride + H2O
?
show the reaction diagram
-
-
-
-
?
hemofiltrate CC chemokine 1 + H2O
[9-74] processed variant of hemofiltrate CC chemokine 1 + ?
show the reaction diagram
IkappaBalpha
?
show the reaction diagram
-
plasmin induces phosphorylation of IkappaBalpha, targeting the inhibitor to proteosomal degradation, consequently allowing nuclear translocation of NF-kappaB
-
-
?
inactive complement component C3b + H2O
?
show the reaction diagram
-
plasmin degrades inactive complement component C3b through cleavage at R945 generating C3dg- and C3c-like species
-
-
?
insulin + H2O
?
show the reaction diagram
-
cleavage of the Arg25-Gly and Lys29-Ala peptide bonds of the beta-chain of oxidized bovine insulin
-
-
?
JAK1
?
show the reaction diagram
-
triggers tyrosine phosphorylation
-
-
?
kappa-casein + H2O
?
show the reaction diagram
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
KKSPGRVVGGSVAH + H2O
KKSPGR + VVGGSVAH
show the reaction diagram
-
-
-
?
KQWK-4-nitroanilide + H2O
KQWK + 4-nitroaniline
show the reaction diagram
-
peptide substrate
-
-
?
KTFK-4-nitroanilide + H2O
KTFK + 4-nitroaniline
show the reaction diagram
-
peptide substrate
-
-
?
L-Ile-Phe-Lys + H2O
?
show the reaction diagram
-
-
-
-
?
lactoferrin + H2O
?
show the reaction diagram
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
Laminin + H2O
?
show the reaction diagram
-
-
-
-
?
LGGSAMSRMSSLE + H2O
LGGSAMSR + MSSLE
show the reaction diagram
-
-
-
?
LGGSGANFRGKLE + H2O
LGGSGANFR + GKLE
show the reaction diagram
-
-
-
?
LGGSGAVYKAGLE + H2O
LGGSGAVYK + AGLE
show the reaction diagram
-
-
-
?
LGGSGIGRSRSLE + H2O
LGGSGIGR + SRSLE
show the reaction diagram
-
-
-
?
LGGSGIYRSRSLE + H2O
LGGSGIYR + SRSLE
show the reaction diagram
-
-
-
?
LGGSGIYRSVSLE + H2O
LGGSGIYR + SVSLE
show the reaction diagram
-
-
-
?
LGGSGIYRVRSLE + H2O
LGGSGIYR + VRSLE
show the reaction diagram
-
-
-
?
LGGSGPYRSRSLE + H2O
LGGSGPYR + SRSLE
show the reaction diagram
-
-
-
?
LGGSGTQRRLRLE + H2O
LGGSGTQR + RLRLE
show the reaction diagram
-
-
-
?
LGGSGYKIGGSLE + H2O
LGGSGYK + IGGSLE
show the reaction diagram
-
-
-
?
LGGSIRYKGKSLE + H2O
LGGSIRYK + GKSLE
show the reaction diagram
-
-
-
?
LGGSSIYRSRSLE + H2O
LGGSSIYR + SRSLE
show the reaction diagram
-
-
-
?
MT1-matrix metalloproteinase + H2O
?
show the reaction diagram
-
-
-
?
N-methyl-D-aspartate receptor NR2A subunit
?
show the reaction diagram
-
plasmin cleaves the native NR2A amino-terminal domain, removing the functional high affinity Zn2+ binding site. Plasmin also cleaves recombinant NR2A amino-terminal domain at lysine 317, thereby producing a 40 kDa fragment, consistent with plasmin-induced NR2A cleavage fragmentsobserved in rat brain preparations. Zn2+ inhibition of agonist-evoked N-methyl-D-aspartate receptor currents of NR1/NR2A-transfected HEK 293 cells and cultured cortical neurons is significantly reduced by plasmin treatment. Mutating the plasmin cleavage site Lys317 on NR2A to alanine blocks plasmins effect on Zn2+ inhibition
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N-Suc-L-Ala-L-Phe-L-Lys-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
N-succinyl-L-alanyl-L-phenylalanyl-L-lysyl-7-amido-4-methylcoumarin + H2O
N-succinyl-L-alanyl-L-phenylalanyl-L-lysine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
osteopontin + H2O
?
show the reaction diagram
p-nitrophenyl-p'-(guanidinium)benzoate + H2O
?
show the reaction diagram
-
-
-
-
?
p-nitrophenyl-p'-(methylethylsulfoniummethyl)benzoate + H2O
?
show the reaction diagram
-
-
-
-
?
p-nitrophenyl-p'-(pyridiniummethyl)-benzoate + H2O
?
show the reaction diagram
-
-
-
-
?
p-nitrophenyl-p'-(thiouroniummethyl)benzoate + H2O
?
show the reaction diagram
-
-
-
-
?
p38 MAPK
?
show the reaction diagram
-
triggers phosphorylation
-
-
?
p65
?
show the reaction diagram
-
triggeres nuclear translocation
-
-
?
plasminogen + H2O
?
show the reaction diagram
platelet-derived growth factor-C + H2O
?
show the reaction diagram
pro-brain-derived neurotrophic factor + H2O
?
show the reaction diagram
-
plasmin is a specific and efficient activator of pro-brain-derived neurotrophic factor. The pro-form is rapidly processed to an 18 kDa fragment at a low concentration of plasmin. This C-terminal fragment is equivalent in size to the furin-processed, mature form of wild-type brain-derived neurotrophic factor. The proteolytic cleavage site is Arg125-Val126, within the consensus furin-cleavage motif
-
-
?
pro-matrix metalloproteinase-1 + H2O
active matrix metalloproteinase-1
show the reaction diagram
-
matrix metalloproteinase-1 activation by the UP A/plasmin system
-
-
?
pro-matrix metalloproteinase-1 + H2O
matrix metalloproteinase-1 + ?
show the reaction diagram
-
-
-
?
pro-matrix metalloproteinase-10 + H2O
matrix metalloproteinase-10 + ?
show the reaction diagram
-
-
-
?
pro-matrix metalloproteinase-13 + H2O
matrix metalloproteinase-13 + ?
show the reaction diagram
-
-
-
?
pro-matrix metalloproteinase-2 + H2O
matrix metalloproteinase-2 + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
show the reaction diagram
pro-matrix metalloproteinase-9 + H2O
matrix metalloproteinase-9 + ?
show the reaction diagram
-
-
-
?
probrain derived neurotrophic factor + H2O
mature brain derived neurotrophic factor
show the reaction diagram
-
-
-
-
?
protamin-heparin complex + H2O
?
show the reaction diagram
-
-
-
-
?
RQFR-4-nitroanilide + H2O
RQFR + 4-nitroaniline
show the reaction diagram
-
peptide substrate
-
-
?
RQWK-4-nitroanilide + H2O
RQWK + 4-nitroaniline
show the reaction diagram
-
peptide substrate
-
-
?
S-2251 + H2O
?
show the reaction diagram
-
-
-
?
S-sulfo-fibrinogen + H2O
?
show the reaction diagram
-
cleaves only Lys and Arg peptide bonds
-
-
?
SPGRVV + H2O
SPGR + Val-Val
show the reaction diagram
-
-
-
?
STAT3
?
show the reaction diagram
-
phosphorylates on Tyr705 and Ser727. Triggeres activation and nuclear translocation of STAT3
-
-
?
Suc-Ala-Phe-Lys-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
thrombin-activatable fibrinolysis inhibitor + H2O
?
show the reaction diagram
-
mutant variants with variants in the amino acids surrounding the scissile R92-A93 bond such as P91S, R92K, and S90P exhibit specific impairment of activation by plasmin
-
-
?
tissue factor pathway inhibitor + H2O
?
show the reaction diagram
-
plasmin increases tissue factor activity by inactivating the cell-associated tissue factor pathway inhibitor by a limited proteolysis
-
-
?
Tosyl-Arg methyl ester + H2O
?
show the reaction diagram
tosyl-Gly-Pro-Lys-4-nitroanilide + H2O
tosyl-Gly-Pro-Lys + 4-nitroaniline
show the reaction diagram
transforming growth factor beta 2 + H2O
?
show the reaction diagram
-
-
-
-
?
TYK2
?
show the reaction diagram
-
triggers tyrosine phosphorylation
-
-
?
vascular endothelial growth factor + H2O
?
show the reaction diagram
VQYK-4-nitroanilide + H2O
VQYK + 4-nitroaniline
show the reaction diagram
-
peptide substrate
-
-
?
VQYR-4-nitroanilide + H2O
VQYR + 4-nitroaniline
show the reaction diagram
-
peptide substrate
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ADAMTS13 + H2O
?
show the reaction diagram
-
inactivation
-
-
?
amyloid-beta + H2O
?
show the reaction diagram
-
the plasmin pathway is induced by aggregated amyloid-beta, which can lead to amyloid-beta degradation and inhibition of amyloid-beta actions
-
?
beta2-glycoprotein I + H2O
?
show the reaction diagram
-
in human plasma beta2-glycoprotein I is proteolytically cleaved by plasmin in its domain V (nicked beta2GPI), resulting in binding to plasminogen
-
-
?
chromogranin A + H2O
hCgA-(360-373) + ?
show the reaction diagram
-
the product hCgA-(360-373) is a bioactive fragment that inhibits nicotinic-mediated catecholamine release. The plasminogen/plasmin system through its interaction with chromogranin A may play a major role in catecholaminergic function
-
?
complement component C3 + H2O
complement component C3a + ?
show the reaction diagram
-
-
-
-
?
complement component C3a + H2O
?
show the reaction diagram
-
-
-
-
?
complement component C3b + H2O
?
show the reaction diagram
-
the enzyme inactivates the C3b molecule for complement C3b amplification
-
-
?
epithelial sodium channel + H2O
epithelial sodium channel gamma subunit + ?
show the reaction diagram
-
-
-
-
?
epithelial sodium channel gamma subunit + H2O
?
show the reaction diagram
-
plasmin activates epithelial sodium channels in association with inducing cleavage of the gamma subunit at gammaLys194, a site distal to the furin site. A gammaK194A mutant epithelial sodium channel subunit prevents both plasmin-dependent activation of epithelial sodium channel and plasmin-dependent production of a unique 70-kDa carboxyl-terminal gamma subunit cleavage fragment
-
-
?
Fibrin + H2O
?
show the reaction diagram
fibrin + H2O
soluble fibrin fragments
show the reaction diagram
P00747
-
-
-
?
Glu-plasminogen + H2O
angiostatin 4.5 (AS4.5)
show the reaction diagram
-
AS4.5 is prepared from Glu-plasminogen by plasmin digestion
-
-
?
hemofiltrate CC chemokine 1 + H2O
[9-74] processed variant of hemofiltrate CC chemokine 1 + ?
show the reaction diagram
-
urokinase plasminogen activator and plasmin efficiently convert hemofiltrate CC chemokine 1 into its active [9-74] processed variant
-
?
inactive complement component C3b + H2O
?
show the reaction diagram
-
plasmin degrades inactive complement component C3b through cleavage at R945 generating C3dg- and C3c-like species
-
-
?
MT1-matrix metalloproteinase + H2O
?
show the reaction diagram
P00747
-
-
-
?
N-methyl-D-aspartate receptor NR2A subunit
?
show the reaction diagram
-
plasmin cleaves the native NR2A amino-terminal domain, removing the functional high affinity Zn2+ binding site. Plasmin also cleaves recombinant NR2A amino-terminal domain at lysine 317, thereby producing a 40 kDa fragment, consistent with plasmin-induced NR2A cleavage fragmentsobserved in rat brain preparations. Zn2+ inhibition of agonist-evoked N-methyl-D-aspartate receptor currents of NR1/NR2A-transfected HEK 293 cells and cultured cortical neurons is significantly reduced by plasmin treatment. Mutating the plasmin cleavage site Lys317 on NR2A to alanine blocks plasmins effect on Zn2+ inhibition
-
-
-
osteopontin + H2O
?
show the reaction diagram
-
osteopontin is cleaved at multiple sites close to its integrin-binding motifs in milk and is a substrate for plasmin and cathepsin D
-
-
?
pro-matrix metalloproteinase-1 + H2O
matrix metalloproteinase-1 + ?
show the reaction diagram
P00747
-
-
-
?
pro-matrix metalloproteinase-10 + H2O
matrix metalloproteinase-10 + ?
show the reaction diagram
P00747
-
-
-
?
pro-matrix metalloproteinase-13 + H2O
matrix metalloproteinase-13 + ?
show the reaction diagram
P00747
-
-
-
?
pro-matrix metalloproteinase-2 + H2O
matrix metalloproteinase-2 + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
show the reaction diagram
P00747
-
-
-
?
pro-matrix metalloproteinase-9 + H2O
matrix metalloproteinase-9 + ?
show the reaction diagram
P00747
-
-
-
?
probrain derived neurotrophic factor + H2O
mature brain derived neurotrophic factor
show the reaction diagram
-
-
-
-
?
tissue factor pathway inhibitor + H2O
?
show the reaction diagram
-
plasmin increases tissue factor activity by inactivating the cell-associated tissue factor pathway inhibitor by a limited proteolysis
-
-
?
vascular endothelial growth factor + H2O
?
show the reaction diagram
-
in non-healing wounds plasmin cleaves and inactivates vascular endothelial growth factor VEGF165
-
?
additional information
?
-
INHIBITORS
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
synthetic construct
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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
synthetic construct
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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
synthetic construct
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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
4-(2-aminoethyl)benzenesulfonyl fluoride
-
-
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
-
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
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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
4-amidinophenyl methane-sulfonyl fluoride
4-aminobenzamidine
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competitive inhibition
4-aminomethylbenzamidine
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competitive inhibition
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4-carboxybenzamidine
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competitive inhibition
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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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6-Aminohexanoic acid
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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Aedes aegypti trypsin inhibitor
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AG490
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JAK inhibitor, inhibits JAK1 but does not inhibit TYK2 phosporylation 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(2)-plasmin inhibitor
alpha-antiplasmin
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potent inhibitor
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alpha-antitrypsin
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alpha-lactalbumin
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shows a strong correlation with plasmin activity and may have inhibitory activity against plasmin
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alpha1 globulin
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alpha1-protease inhibitor
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plasmin bound to fibrin is completely protected
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alpha2 globulin
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alpha2-antiplasmin
alpha2-Macroglobulin
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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Amino methyl cyclohexane carboxylic acid
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amyloid precursor-like protein 2
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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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Aprotinin
arachidonate
synthetic construct
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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
bdellin
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benzamidine
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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bikazin salivary inhibitor
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bikunin
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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 (70C 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
-
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
chicken liver trypsin inhibitor
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Cholesterol sulfate
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reduces plasmin activity in a dose-dependent manner
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
CU-2010
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potent inhibitpr
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D-Ile-Phe-Lys
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D-Ile-Phe-Lys-CH2Cl
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D-Ile-Phe-Lys-CN
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D-Ile-Phe-Lys-NH2
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D-Leu-Lys-benzylamide
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weak inhibitor of amidolytic activity
D-Phe-Lys-benzylamide
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inhibition of fibrinolytic activity, no inhibition of amidolytic activity
D-Val-Phe-Lys-chloromethyl ketone
synthetic construct
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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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DX-1000
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elaidic acid
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60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
epsilon-aminocaprioic acid
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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
Fibrin
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inhibits hydrolysis of D-Val-Leu-Lys-p-nitroanilide
fibrinogen
fragment X
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competitive inhibitor of plasmin chromogenic activity
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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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human aprotinin analogue
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human plasma protein inhibitors
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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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infestin
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KD1-L17R
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KM(O2)YR-H
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Kunitz-type inhibitor 2
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L-Ile-Phe-Lys
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L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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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
Leucaena-type trypsin inhibitor
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Leupeptin
synthetic construct
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inhibits the ability of plasmin to potentiate lipopolysaccharide signalling
Lima bean trypsin inhibitor
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Lys-Met(sulfone)-Tyr-Arg
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shows 25fold selectivity for plasmin over plasma kallikrein
mAb413
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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
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MG-132
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prevents facilitation of degradation of Bim(EL) by plasmin in hepatocytes from mice pretreated with cycloheximide
MgCl2
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0.01 M and above
N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzyloxycarbonyl)-octylamide
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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
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molecular modeling
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-1-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
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N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-2-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
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N-[(1S)-5-amino-1-cyanopentyl]-3-[[(4-fluorophenyl)acetyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
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N-[(1S)-5-amino-1-cyanopentyl]-3-[[3-(1H-indol-3-yl)propanoyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
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N-[(1S)-5-amino-1-cyanopentyl]-4-(pyridin-4-ylmethoxy)benzamide
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1-glycyl-4-oxopyrrolidin-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclohexyl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclopentyl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobenzyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobutyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-tryptophanamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(5-aminopentyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(7-aminoheptyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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N-[(benzyloxy)carbonyl]-L-tryptophyl-N-[(trans-4-aminocyclohexyl)methyl]-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
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Nalpha-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-N-hexyl-O-(pyridin-4-ylmethyl)-L-tyrosinamide
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binding mode
natural aprotinin
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neuroserpin
nexin 2
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Nomega-nitro-L-arginine methyl ester
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almost completely abolishes plasmin-induced relaxation
oleate
synthetic construct
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oleic acid
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59% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
ONO-3307
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i.e. 4-sulfamoyl phenyl-4-guanidinobenzoate methanesulfonate
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Pancreatic trypsin inhibitor
PD98059
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MEK inhibitor, completely abolishes plasmin-induced phosphorylation of ERK1/2 at 0.05 mM
pefabloc
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Pentamidine
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competitive inhibition
peptide GHRPYam
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delays appearance of plasmin activity
peroxynitrite
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50% inhibition at 280 microM and an enzyme concentration of 10 microM
Phe-Lys-benzylamide
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inhibition of fibrinolytic activity, no inhibition of amidolytic activity
PKSI-527
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plasminogen activator inhibitor 1
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plasminogen activator inhibitor I
plasminogen activator inhibitor II
plasminogen activator inhibitor-type 1
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totally blocks plasmin activity and degradation of casein
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plasminogen activator inhibitors 1
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plasminogen activator inhibitors 2
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plasminostreptin
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Protein C inhibitor
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from Bos taurus
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R484A mutant of A2
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subunit of factor VIII, possessing ca. 250fold reduced affinity for plasmin, weakly inhibits factor VIIIa inactivation by ca. 20%
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recombinant aprotinin
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RG1192
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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
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RG1503
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SB203580
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inhibits plasmin-induced TNF-alpha release by 75% and IL-6 release by 79%
serpinb2
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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
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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
-
Soybean trypsin inhibitor
stearate
synthetic construct
-
-
streptokinase
-
-
-
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
-
-
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-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
-
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
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Aprotinin
-
augments binding of hepatocytes from mice to immobilized plasmin
arachidonate
synthetic construct
-
-
Blood serum
-
2.0% equine serum increases plasmin activity by ca.50% when assayed with N-Suc-L-Ala-L-Phe-L-Lys-7-amido-4-methyl-coumarin in milk
-
Efb protein
-
plasminogen bound to Efb protein is converted to plasmin
-
Factor IXa
-
regulates plasmin-catalyzed factor VIIIa inactivation
-
fragment X
-
profibrinolytic effect with plasmin. Rates of plasmin formation increase with increasing fragment X concentrations. Plasmin degrades clots containing fragment X more rapidly than fibrin clots
-
high molecular weight urokinase-type plasminogen activator
-
induces a significant increase in plasmin activity in unstimulated or lipopolysaccharide-stimulated monocytes
-
low molecular weight urokinase-type plasminogen activator
-
induces a significant increase in plasmin activity in unstimulated or lipopolysaccharide-stimulated monocytes
-
oleate
synthetic construct
-
-
Sbi protein
-
plasminogen bound to Sbi protein is converted to plasmin
-
stearate
synthetic construct
-
-
tissue plasminogen activator
-
-
-
urokinase plasminogen activator1
-
-
-
urokinase-type plasminogen activator
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.003
AIYRSR
-
pH 8.0
0.0135 - 0.083
benzyloxycarbonyl-Lys-p-nitrophenyl ester
0.004
CIYRSR
-
pH 8.0
0.02
D-Ile-Phe-Lys
-
pH and temperature not specified in the publication
0.00589 - 0.1311
D-norleucyl-hexahydrotyrosyl-lysine-p-nitroanilide
0.138 - 0.325
D-Val-L-Leu-L-Lys-4-nitroanilide
0.21 - 1.26
D-Val-Leu-Lys-p-nitroanilide
0.03
fibrinogen
-
-
-
0.012
GIVRSR
-
pH 8.0
0.002 - 0.0058
GIYRSR
0.0047
GPGRVV
-
pH 8.0
0.00076
hemofiltrate CC chemokine 1
-
-
-
5.1
KKSPGRVVGGSVAH
-
pH 8.0
0.33
L-Ile-Phe-Lys
-
pH and temperature not specified in the publication
1.6
LGGSAMSRMSSLE
-
pH 8.0
2.4
LGGSGANFRGKLE
-
pH 8.0
0.42
LGGSGAVYKAGLE
-
pH 8.0
1.85
LGGSGIGRSRSLE
-
pH 8.0
0.1
LGGSGIYRSRSLE
-
pH 8.0
3.7
LGGSGIYRSVSLE
-
pH 8.0
0.47
LGGSGIYRVRSLE
-
pH 8.0
1.7
LGGSGPYRSRSLE
-
pH 8.0
2.9
LGGSGTQRRLRLE
-
pH 8.0
0.21
LGGSGYKIGGSLE
-
pH 8.0
0.75
LGGSIRYKGKSLE
-
pH 8.0
6.8
LGGSSIYRSRSLE
-
pH 8.0
0.0052 - 0.0113
p-nitrophenyl-p'-(guanidinium)benzoate
0.214 - 0.258
p-nitrophenyl-p'-(methylethylsulfoniummethyl)benzoate
0.21 - 0.23
p-nitrophenyl-p'-(pyridiniummethyl)-benzoate
0.027 - 0.043
p-nitrophenyl-p'-(thiouroniummethyl)benzoate
0.021
p-tosyl-Arg methyl ester
-
-
0.036
SPGRVV
-
pH 8.0
0.005
thrombin-activatable fibrinolysis inhibitor
-
-
-
5.3 - 7
tosyl-Arg methyl ester
additional information
additional information
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.036
AIYRSR
Homo sapiens
-
pH 8.0
2.1 - 22.3
benzyloxycarbonyl-Lys-p-nitrophenyl ester
2.7
CIYRSR
Homo sapiens
-
pH 8.0
12.6 - 12.97
D-Val-L-Leu-L-Lys-4-nitroanilide
14.5 - 25.7
D-Val-Leu-Lys-p-nitroanilide
0.039
GIVRSR
Homo sapiens
-
pH 8.0
0.6 - 1.5
GIYRSR
0.0016
GPGRVV
Homo sapiens
-
pH 8.0
6
hemofiltrate CC chemokine 1
Homo sapiens
-
-
-
0.0086
KKSPGRVVGGSVAH
Homo sapiens
-
pH 8.0
3.2
LGGSAMSRMSSLE
Homo sapiens
-
pH 8.0
68
LGGSGANFRGKLE
Homo sapiens
-
pH 8.0
40
LGGSGAVYKAGLE
Homo sapiens
-
pH 8.0
53
LGGSGIGRSRSLE
Homo sapiens
-
pH 8.0
120
LGGSGIYRSRSLE
Homo sapiens
-
pH 8.0
39
LGGSGIYRSVSLE
Homo sapiens
-
pH 8.0
16
LGGSGIYRVRSLE
Homo sapiens
-
pH 8.0
92
LGGSGPYRSRSLE
Homo sapiens
-
pH 8.0
12
LGGSGTQRRLRLE
44
LGGSIRYKGKSLE
Homo sapiens
-
pH 8.0
35
LGGSSIYRSRSLE
Homo sapiens
-
pH 8.0
0.125
p-nitrophenyl-p'-(guanidinium)benzoate
Oryctolagus cuniculus
-
plasmin 1 and plasmin 2
-
0.117 - 0.144
p-nitrophenyl-p'-(methylethylsulfoniummethyl)benzoate
0.122 - 0.127
p-nitrophenyl-p'-(pyridiniummethyl)-benzoate
0.333 - 0.364
p-nitrophenyl-p'-(thiouroniummethyl)benzoate
0.039
SPGRVV
Homo sapiens
-
pH 8.0
0.00042
thrombin-activatable fibrinolysis inhibitor
Homo sapiens
-
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.051 - 0.061
4-aminobenzamidine
1.074 - 1.408
4-aminomethylbenzamidine
0.292 - 0.301
4-carboxybenzamidine
0.0057
479-504 peptide of factor VIII
-
-
-
0.0103
484-509 peptide of factor VIII
-
-
-
0.0628
489-514 peptide of factor VIII
-
-
-
0.0068 - 0.0113
6-Aminohexanoic acid
0.0000038
Aedes aegypti trypsin inhibitor
-
pH and temperature not specified in the publication
-
0.000081
amyloid precursor-like protein 2
-
pH and temperature not specified in the publication
-
0.00000018
Aprotinin
-
pH and temperature not specified in the publication
0.00000156
bdellin
-
pH and temperature not specified in the publication
-
0.032 - 0.161
benzamidine
0.002
bikazin salivary inhibitor
-
pH and temperature not specified in the publication
-
0.0001
bikunin
-
pH and temperature not specified in the publication
-
0.000127
chicken liver trypsin inhibitor
-
pH and temperature not specified in the publication
-
0.0000022
CU-2010
-
pH and temperature not specified in the publication
-
0.00057
D-Ile-Phe-Lys-CH2Cl
-
pH and temperature not specified in the publication
-
0.000000087
DX-1000
-
pH and temperature not specified in the publication
-
0.0038
fibrinogen
-
-
-
0.0095
fragment X
-
-
-
0.0000227
human aprotinin analogue
-
compared with recombinant-aprotinin, the Ki of the human aprotinin analogue is found to increase by about 2.6fold, suggesting that the substitution of Arg17-Ile18 with Lys17-Met18 in aprotinin somehow impair its interaction with plasmin
-
0.0000011
infestin
-
pH and temperature not specified in the publication
-
0.0000009
KD1-L17R
-
pH and temperature not specified in the publication
-
0.0000031
KM(O2)YR-H
-
pH and temperature not specified in the publication
-
0.00000104
Kunitz-type inhibitor 2
-
pH and temperature not specified in the publication
-
0.000027
LEKTI
-
-
0.00000032
Leucaena-type trypsin inhibitor
-
pH and temperature not specified in the publication
-
0.0000031
Lys-Met(sulfone)-Tyr-Arg
-
pH 8.0, 22C
0.0000075
natural aprotinin
-
-
-
0.000042
nexin 2
-
pH and temperature not specified in the publication
-
0.00033
ONO-3307
-
pH and temperature not specified in the publication
-
0.0022 - 0.004
Pentamidine
0.00000049
plasminostreptin
-
pH and temperature not specified in the publication
-
0.00015
Protein C inhibitor
-
37C
-
0.0000086
recombinant aprotinin
-
-
-
0.000028
RG1192
-
pH 7.4, 37C
-
0.00011
RG1503
-
pH 7.4, 37C
-
0.0002 - 0.0025
stearate
0.000055
TdPI tryptase inhibitor
-
pH and temperature not specified in the publication
-
0.0000035
textilinin-1
0.000026
tissue factor pathway inhibitor-1
-
pH and temperature not specified in the publication
-
0.00001
tissue factor pathway inhibitor-2
-
pH and temperature not specified in the publication
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.062
(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
synthetic construct
-
-
0.025
(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
synthetic construct
-
-
0.63
(4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-phenyl-propionylamino]-phenyl)-acetic acid
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.63 mM
0.3
(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
synthetic construct
-
-
0.024
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
Homo sapiens
-
IC50: 0.024 mM
0.0042
2-[(4-Aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionic acid pyridin-2-ylmethyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0042 mM
0.02
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
Homo sapiens
-
IC50: 0.02 mM
0.0039
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.024 mM, IC50 in reaction with fibrin is 0.0039 mM
0.0043
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid hexyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.018 mM, IC50 in reaction with fibrin is 0.0043 mM
0.0061
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid methyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0009 mM, IC50 in reaction with fibrin is 0.0061 mM
0.005
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid octyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is above 0.1 mM, IC50 in reaction with fibrin is 0.005 mM
0.00042
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0014 mM, IC50 in reaction with fibrin is 0.00042 mM
0.0004
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid hexyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0015 mM, IC50 in reaction with fibrin is 0.0004 mM
0.00078
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid methyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.001 mM, IC50 in reaction with fibrin is 0.00078 mM
0.00056
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid octyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0025 mM, IC50 in reaction with fibrin is 0.00056 mM
0.000151
Ah-plasmin
Homo sapiens
-
-
-
0.0012
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0062 mM, IC50 in reaction with fibrin is 0.0012 mM
0.0033
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-heptylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.011 mM, IC50 in reaction with fibrin is 0.0033 mM
0.0027
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-hexylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.013 mM, IC50 in reaction with fibrin is 0.0027 mM
0.0013
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-nonylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0083 mM, IC50 in reaction with fibrin is 0.0013 mM
0.0018
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-octylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.007 mM, IC50 in reaction with fibrin is 0.0018 mM
0.0013
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-pentylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.01 mM, IC50 in reaction with fibrin is 0.0013 mM
0.019
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.085 mM, IC50 in reaction with fibrin is 0.019 mM
0.0023
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-butyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.009 mM, IC50 in reaction with fibrin is 0.0023 mM
0.0035
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-hexyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.006 mM, IC50 in reaction with fibrin is 0.0035 mM
0.0047
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-pentyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.009 mM, IC50 in reaction with fibrin is 0.0047 mM
0.002
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-propylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0092 mM, IC50 in reaction with fibrin is 0.002 mM
0.0017
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.013 mM, IC50 in reaction with fibrin is 0.0017 mM
0.000056
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(3-methyl-butylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00046 mM, IC50 in reaction with fibrin is 0.000056 mM
0.00009
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-butyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00079 mM, IC50 in reaction with fibrin is 0.00009 mM
0.000098
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-ethyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00063 mM, IC50 in reaction with fibrin is 0.000098 mM
0.00024
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-hexyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00049 mM, IC50 in reaction with fibrin is 0.00024 mM
0.00007
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-pentyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00057 mM, IC50 in reaction with fibrin is 0.00007 mM
0.00017
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(pyridin-4-ylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00098 mM, IC50 in reaction with fibrin is 0.00017 mM
0.00043
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-heptylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.00043 mM
0.00038
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-hexylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0012 mM, IC50 in reaction with fibrin is 0.00038 mM
0.0001
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-nonylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
0.00052
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[(pyridin-2-ylmethyl)-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0015 mM, IC50 in reaction with fibrin is 0.00052 mM
0.0014
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[(pyridin-4-ylmethyl)-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is0.0053 mM, IC50 in reaction with fibrin is 0.0014 mM
0.0003
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[benzyl-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
Homo sapiens
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.0003 mM
0.02
D-Ile-Phe-Lys
Homo sapiens
-
pH and temperature not specified in the publication
0.078
D-Ile-Phe-Lys-CN
Homo sapiens
-
pH and temperature not specified in the publication
0.29
D-Ile-Phe-Lys-NH2
Homo sapiens
-
pH and temperature not specified in the publication
0.33
L-Ile-Phe-Lys
Homo sapiens
-
pH and temperature not specified in the publication
0.375
L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.0008
N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzyloxycarbonyl)-octylamide
Homo sapiens
-
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
0.14
N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-(pyridin-4-ylmethoxy)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.57
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-1-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.22
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-2-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.59
N-[(1S)-5-amino-1-cyanopentyl]-3-[[(4-fluorophenyl)acetyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.37
N-[(1S)-5-amino-1-cyanopentyl]-3-[[3-(1H-indol-3-yl)propanoyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.24
N-[(1S)-5-amino-1-cyanopentyl]-4-(pyridin-4-ylmethoxy)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.013
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.35
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1-glycyl-4-oxopyrrolidin-3-yl)-L-phenylalaninamide
synthetic construct
-
-
1
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclohexyl)-L-phenylalaninamide
0.019
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobenzyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.14
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobutyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.022
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.03
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-tryptophanamide
synthetic construct
-
-
0.1
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(5-aminopentyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.0057
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
synthetic construct
-
one of the most effective inhibitors
0.009
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
one of the most effective inhibitors
0.051
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(7-aminoheptyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.054
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-[(trans-4-aminocyclohexyl)methyl]-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
synthetic construct
-
-
0.00053
Nalpha-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-N-hexyl-O-(pyridin-4-ylmethyl)-L-tyrosinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.63
PKSI-527
Homo sapiens
-
pH and temperature not specified in the publication
-
0.22
tert-butyl 3-(3-[[5-[[(1S)-5-amino-1-cyanopentyl]carbamoyl]-2-(pyridin-4-ylmethoxy)phenyl]amino]-3-oxopropyl)-1H-indole-1-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00054
Tra-Tyr(O-Pic)-CONH-(C6H6)-(CH2)4-CH3
Homo sapiens
-
pH and temperature not specified in the publication
-
0.0017
Tra-Tyr(O-Pic)-CONH-(C6H6)-CH2-CH3
Homo sapiens
-
pH and temperature not specified in the publication
-
0.0019
Tra-Tyr(O-Pic)-CONH-(CH2)2-CH(CH3)-CH3
Homo sapiens
-
pH and temperature not specified in the publication
-
0.0055
Tra-Tyr(O-Pic)-CONH-(CH2)7-COOH
Homo sapiens
-
pH and temperature not specified in the publication
-
0.0038
Tra-Tyr(O-Pic)-CONH-(CH2)7-NH2
Homo sapiens
-
pH and temperature not specified in the publication
-
0.00053
YO-2
Homo sapiens
-
pH and temperature not specified in the publication
-
0.65
[4-[(N-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-L-phenylalanyl)amino]phenyl]acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
electrochemical assay and properties of plasmin adsorbed onto a carbon paste electrode
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
7.4 - 8
-
assay at
7.4
-
assay at
7.5
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.8 - 6.6
-
-
7.5 - 9.5
-
pH 7.5: about 40% of maximal activity, pH 9.5: about 50% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22 - 37
-
assay at 37C or at room temperature
37
-
assay at
37 - 45
-
-
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
plasmin is generated by the plasmin/u-PA system on surfaces of A-549 alveolar lining cells
Manually annotated by BRENDA team
-
vessel wall
Manually annotated by BRENDA team
-
plasmin evokes an increase in both phosphoinositide hydrolysis and Fura-2/AM fluorescence in cultured cortical astrocytes. Plasmin activiates extracellular signal-regulated kinase and induces a rise in intracellular Ca2+ concentration and phopho-ERK1/2 levels
Manually annotated by BRENDA team
-
plasmin has no effect on ERK1/2 signaling or Ca2+ concentraion in primary cultured hippocampal neurons or hippocampal slices
Manually annotated by BRENDA team
-
originally isolated from a cirrhotic liver
Manually annotated by BRENDA team
-
plasmin induces scattering of HT-29-M6 cells in the presence of 12-myristate 13-acetate
Manually annotated by BRENDA team
-
plasmin induces a concentration-dependent transient elevation in the cytosolic Ca2+ concentrations
Manually annotated by BRENDA team
-
leukaemic cell line. In L5178Y cells with knock-out of the gene for annexin A2, the mRNA level of plasminogen is not substantially changed, but the protein level of plasmin is significantly lowered. mRNA and protein levels of S100A10 and fascin are lower in annexin A2 knock-out cells than in wild-type L5178Y cells
Manually annotated by BRENDA team
-
plasmin triggers expression and release of proinflammatory cytokines such as TNF-alpha and IL-6 in human monocyte-derived macrophages with a somewhat lower potency than the standard stimulus lipopolysaccharide. Plasmin-induced activation of JAK1, p38, ERK1/2, and NF-kappaB is indispensable for the cytokine expression
Manually annotated by BRENDA team
-
in CA1 pyramidal neuron, plasmin application potentiates the N-methyl-D-aspartate receptor-dependent component of miniature excitatory postsynaptic currents recorded from CA1 pyramidal neurons but has no effect on -amino-3-hydroxy-5-methyl-4-isoxazole propionate- or -aminobutyric acid receptor-mediated synaptic currents. Plasmin also increased N-methyl-D-aspartate-induced whole cell receptor currents recorded from CA1 pyramidal cells
Manually annotated by BRENDA team
-
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
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
plasminogen is a major surface-bound protein
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
75400
-
equilibrium sedimentation
82000 - 84000
-
enzyme inactivated with diisopropyl fluorophosphate, enzyme form F-2, high speed analytical ultracentrifugation
83000 - 86000
-
enzyme inactivated with diisopropyl fluorophosphate, enzyme form F-1, high speed analytical ultracentrifugation
85000
-
-
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
the human plasminogen is partially N-glycosylated at Asn289 and O-glycosylated at Ser249 and Thr346 giving rise to plasminogen variants I (Asn289, Thr346) and II (only Thr346)
phosphoprotein
plasminogen is partially phosphorylated at Ser578
proteolytic modification
side-chain modification
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
crystal structure of plasmin complexed with streptokinase
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4
-
very stable below
95552
7
-
unstable in absence of glycerol
95552
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
56
-
rapid destruction or inactivation
65
-
denaturation above 65C, thermal stability of plasmin in milk is very much dependent upon its interaction with beta-lactoglobulin
90
-
stable for 108 min in acid whey and 0.02 min in sweet whey
95
-
pasteurization of whey protein-free retentate of micro- and difiltrated milk at 95C for 15 s does not significantly affect plasmin or plasminogen-derived activities. The retentate contains increased plasmin activity, proportional to the concentration of beta-lactoglobulin
additional information
-
the increased activity of plasmin after heat treatment may be also due to inactivation of enzyme inhibitor proteins
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
freezing and thawing results in loss of activity
-
plasmin-staphylokinase complex is more stable than plasmin(ogen)-streptokinase complex
-
reduction with 2-mercaptoethanol in 8 M urea at pH 9.0, complete loss of activity by cleavage of a single disulfide bond
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20C to -30C, pH 9.0, Tris-Lys-NaCl-EDTA buffer containing 25% glycerol, stable
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
affinity chromatography
-
enzyme form F-1 and enzyme form F-2
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
-
mutant enzyme P611I expressed in recombinant baculovirus-infected Spodoptera frugiperda cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
plasminogen levels ae significantly higher in Cardiac neonatal lupus compared with non-cardiac neonatal lupus children
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
P611I
-
mutant enzyme has no amidolytic activity with D-Val-Leu-Lys-p-nitroanilide
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
agriculture
-
effect of plasmin on in vitro embryo production. Plasmin added to the 18 h in vitro maturation medium increases the maturation rate of embryos without affecting fertilization or embryo development rates
analysis
-
electrochemical assay of plasmin activity based on a ferrocenyl peptide substrate having a plasmin-specific substrate sequence, Lys-thr-Phe-Lys, and immobilized on a gold electrode. Detection limit for plasmin is around 50 ng/ml or 0.15 mU/ml. Ratio of kcat/Km values is 0.063 microM/s
degradation
-
cleavage at Arg336 is a central mechanism of plasmin-catalyzed factor VIII inactivation. Cleavages at Arg336 and Lys36 are selectively regulated by the A2 and A3-C1-C2 domains, respectively, interacting with plasmin
food industry
-
milk retentate with increased plasmin activity is an interesting starting material for cheese-making. Increased plasmin activity increases cheese flavour and decreases ripening time
medicine
nutrition
-
hydrolysis of milk proteins alphaS-casein, beta-casein, kappa-casein, alpha-lactalbumin, beta-lactoglobulin, and lactoferrin is highly dependent on photooxidation state of substrate. Changes in the formation of potential angiotensin I-converting enzyme-inhibitory peptides as well as peptides proposed to have anti-bactericidal activities are observed after oxidation of substrates before plasmin hydrolysis
pharmacology
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