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4-nitrophenyl-4'-(guanidinium)benzoate + H2O
?
-
-
-
-
?
4-nitrophenyl-p'-(guanidinium)benzoate bromide + H2O
?
-
-
-
-
?
Ac-FM(O2)YK-4-nitroanilide + H2O
Ac-FM(O2)YK + 4-nitroaniline
-
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
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
Ac-KM(O2)YR + H2O
?
-
-
-
?
Ac-KM(O2)YR-4-nitroanilide + H2O
Ac-KM(O2)YR + 4-nitroaniline
-
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
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
Ac-RM(O2)YR + H2O
?
-
-
-
?
Ac-RM(O2)YR-4-nitroanilide + H2O
Ac-RM(O2)YR + 4-nitroaniline
-
peptide substrate, M(O2) i.e. L-methionine sulfone
M(O2) i.e. L-methionine sulfone
-
?
AIYRSR + H2O
AIYR + Ser-Arg
-
-
-
?
alpha-lactalbumin + H2O
?
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
alphaS-casein + H2O
?
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
alphas1-casein + H2O
?
-
-
-
-
?
amyloid beta peptide Abeta42 + H2O
?
-
cleavage prevents the aggregation of Abeta42 and its cleavage products into beta-pleated sheet structure
-
?
benzyloxycarbonyl-Lys-p-nitrophenyl ester + H2O
?
-
-
-
-
?
beta-lactoglobulin + H2O
?
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
beta2-glycoprotein I + H2O
?
-
in human plasma beta2-glycoprotein I is proteolytically cleaved by plasmin in its domain V (nicked beta2GPI), resulting in binding to plasminogen
-
-
?
Boc-Glu-Lys-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Glu-Lys-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
Boc-Val-Leu-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
C1 inhibitor + H2O
?
-
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
-
?
cadherin + H2O
?
-
plasmin bound to pneumococci is able to cleave recombinant vascular endothelial cadherin
-
-
?
carboxypeptidase N + H2O
?
-
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
-
-
?
chromogenic substrate S-2551 + H2O
?
-
-
-
?
chromogranin A + H2O
catestatin + ?
-
chromogranin A-wild-type, chromogranin A-Gly364Ser and chromogranin A-Arg374Gln completely digested with plasmin at 0.0004 mM
-
-
?
chromogranin A + H2O
hCgA-(360-373) + ?
chromozyme PL + H2O
?
-
-
-
-
?
CIYRSR + H2O
CIYR + Ser-Arg
-
-
-
?
complement component C3 + H2O
complement component C3a + ?
-
-
-
-
?
complement component C3a + H2O
?
-
-
-
-
?
complement component C3b + H2O
?
complement component C5 + H2O
?
-
cleavage by plasmin produces bands of approximately 41000 Da and 30000-28000 Da
-
-
?
D-Ile-Phe-Lys + H2O
?
-
-
-
-
?
D-Nle-hexa-hydrotyrosyl-Lys-4-nitroanilide + H2O
D-Nle-hexa-hydrotyrosyl-Lys + 4-nitroaniline
-
-
-
?
D-Nle-hexahydrotyrosyl-Lys-4-nitroanilide + H2O
D-Nle-hexahydrotyrosyl-Lys + 4-nitroaniline
-
-
-
?
D-norleucyl-hexahydrotyrosyl-lysine-p-nitroanilide + H2O
?
-
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
D-Val-Leu-Lys-p-nitroanilide + H2O
?
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
D-valyl-L-leucyl-L-lysine-4-nitroanilide + H2O
?
-
-
-
-
?
D-valyl-L-leucyl-L-lysine-4-nitroanilide + H2O
D-valyl-L-leucyl-L-lysine + 4-nitroaniline
-
-
-
-
?
epithelial sodium channel + H2O
epithelial sodium channel gamma subunit + ?
-
-
-
-
?
epithelial sodium channel gamma subunit + H2O
?
-
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
-
-
?
ERK1/2
?
-
triggers activation
-
-
?
fibrin + H2O
soluble fibrin fragments
fibrinogen + H2O
fragment X
-
fragment X generated by limited plasmin digestion of fibrinogen
-
-
?
Fibronectin + H2O
?
-
-
-
-
?
GIVRSR + H2O
GIVR + Ser-Arg
-
-
-
?
GIYRSR + H2O
GIYR + Ser-Arg
-
-
-
?
Glu-plasminogen + H2O
angiostatin 4.5 (AS4.5)
-
AS4.5 is prepared from Glu-plasminogen by plasmin digestion
-
-
?
GPGRVV + H2O
GPGR + Val-Val
-
-
-
?
H-D-norleucyl-hexahydrotyrosol-lysine-para nitroanilide diacetate + H2O
?
-
-
-
-
?
H-D-Val-Leu-Lys-p-nitroaniline dihydrochloride + H2O
?
-
-
-
-
?
hemofiltrate CC chemokine 1 + H2O
[9-74] processed variant of hemofiltrate CC chemokine 1 + ?
IkappaBalpha
?
-
plasmin induces phosphorylation of IkappaBalpha, targeting the inhibitor to proteosomal degradation, consequently allowing nuclear translocation of NF-kappaB
-
-
?
inactive complement component C3b + H2O
?
-
plasmin degrades inactive complement component C3b through cleavage at R945 generating C3dg- and C3c-like species
-
-
?
insulin + H2O
?
-
cleavage of the Arg25-Gly and Lys29-Ala peptide bonds of the beta-chain of oxidized bovine insulin
-
-
?
JAK1
?
-
triggers tyrosine phosphorylation
-
-
?
kappa-casein + H2O
?
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
KKSPGRVVGGSVAH + H2O
KKSPGR + VVGGSVAH
-
-
-
?
KQWK-4-nitroanilide + H2O
KQWK + 4-nitroaniline
-
peptide substrate
-
-
?
KTFK-4-nitroanilide + H2O
KTFK + 4-nitroaniline
-
peptide substrate
-
-
?
L-Ile-Phe-Lys + H2O
?
-
-
-
-
?
lactoferrin + H2O
?
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
Laminin + H2O
?
-
-
-
-
?
LGGSAMSRMSSLE + H2O
LGGSAMSR + MSSLE
-
-
-
?
LGGSGANFRGKLE + H2O
LGGSGANFR + GKLE
-
-
-
?
LGGSGAVYKAGLE + H2O
LGGSGAVYK + AGLE
-
-
-
?
LGGSGIGRSRSLE + H2O
LGGSGIGR + SRSLE
-
-
-
?
LGGSGIYRSRSLE + H2O
LGGSGIYR + SRSLE
-
-
-
?
LGGSGIYRSVSLE + H2O
LGGSGIYR + SVSLE
-
-
-
?
LGGSGIYRVRSLE + H2O
LGGSGIYR + VRSLE
-
-
-
?
LGGSGPYRSRSLE + H2O
LGGSGPYR + SRSLE
-
-
-
?
LGGSGTQRRLRLE + H2O
LGGSGTQR + RLRLE
-
-
-
?
LGGSGYKIGGSLE + H2O
LGGSGYK + IGGSLE
-
-
-
?
LGGSIRYKGKSLE + H2O
LGGSIRYK + GKSLE
-
-
-
?
LGGSSIYRSRSLE + H2O
LGGSSIYR + SRSLE
-
-
-
?
Lys-Thr-Phe-Lys-Gly-Gly-Gly-Gly-Gly-Gly-Cys + H2O
Lys-Thr-Phe-Lys + Gly-Gly-Gly-Gly-Gly-Gly-Cys
-
-
-
-
?
MT1-matrix metalloproteinase + H2O
?
-
-
-
?
N-methyl-D-aspartate receptor NR2A subunit
?
-
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
-
-
?
N-Suc-L-Ala-L-Phe-L-Lys-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
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
-
-
-
-
?
p-nitrophenyl-p'-(methylethylsulfoniummethyl)benzoate + H2O
?
-
-
-
-
?
p-nitrophenyl-p'-(pyridiniummethyl)-benzoate + H2O
?
-
-
-
-
?
p-nitrophenyl-p'-(thiouroniummethyl)benzoate + H2O
?
-
-
-
-
?
p38 MAPK
?
-
triggers phosphorylation
-
-
?
p65
?
-
triggeres nuclear translocation
-
-
?
platelet-derived growth factor-C + H2O
?
pro-brain-derived neurotrophic factor + H2O
?
-
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
-
matrix metalloproteinase-1 activation by the UP A/plasmin system
-
-
?
pro-matrix metalloproteinase-1 + H2O
matrix metalloproteinase-1 + ?
-
-
-
?
pro-matrix metalloproteinase-10 + H2O
matrix metalloproteinase-10 + ?
-
-
-
?
pro-matrix metalloproteinase-13 + H2O
matrix metalloproteinase-13 + ?
-
-
-
?
pro-matrix metalloproteinase-2 + H2O
matrix metalloproteinase-2 + ?
-
-
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
pro-matrix metalloproteinase-9 + H2O
matrix metalloproteinase-9 + ?
-
-
-
?
probrain derived neurotrophic factor + H2O
mature brain derived neurotrophic factor
-
-
-
-
?
protamin-heparin complex + H2O
?
-
-
-
-
?
RQFR-4-nitroanilide + H2O
RQFR + 4-nitroaniline
-
peptide substrate
-
-
?
RQWK-4-nitroanilide + H2O
RQWK + 4-nitroaniline
-
peptide substrate
-
-
?
S-sulfo-fibrinogen + H2O
?
-
cleaves only Lys and Arg peptide bonds
-
-
?
Spectrozyme PL + H2O
L-norleucyl-L-hexahydrotyrosyl-L-lysine + 4-nitroaniline
-
i.e. L-norleucyl-L-hexahydrotyrosyl-L-lysine-4-nitroanilide
-
-
?
SPGRVV + H2O
SPGR + Val-Val
-
-
-
?
STAT3
?
-
phosphorylates on Tyr705 and Ser727. Triggeres activation and nuclear translocation of STAT3
-
-
?
Suc-Ala-Phe-Lys-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
thrombin-activatable fibrinolysis inhibitor + H2O
?
-
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
?
-
plasmin increases tissue factor activity by inactivating the cell-associated tissue factor pathway inhibitor by a limited proteolysis
-
-
?
Tosyl-Arg methyl ester + H2O
?
tosyl-Gly-Pro-Lys-4-nitroanilide + H2O
tosyl-Gly-Pro-Lys + 4-nitroaniline
transforming growth factor beta 2 + H2O
?
-
-
-
-
?
TYK2
?
-
triggers tyrosine phosphorylation
-
-
?
vascular endothelial growth factor + H2O
?
von Willebrand factor + H2O
?
-
the enzyme cleaves von Willebrand factor at K1491-R149. Globular von Willebrand factor is resistant to plasmin cleavage under static conditions, but is readily cleaved by plasmin under shear
-
-
?
VQYK-4-nitroanilide + H2O
VQYK + 4-nitroaniline
-
peptide substrate
-
-
?
VQYR-4-nitroanilide + H2O
VQYR + 4-nitroaniline
-
peptide substrate
-
-
?
additional information
?
-
ADAMTS13 + H2O
?
-
-
-
-
?
ADAMTS13 + H2O
?
-
inactivation
-
-
?
amyloid-beta + H2O
?
-
plasmin cleaves at multiple sites
-
?
amyloid-beta + H2O
?
-
the plasmin pathway is induced by aggregated amyloid-beta, which can lead to amyloid-beta degradation and inhibition of amyloid-beta actions
-
?
annexin A2 + H2O
?
-
interaction of plasmin with annexin A2 results in the stimulation of ERK1/2 and p38 MAPK, cyclooxygenase-2, and PGE(2), leading to increased matrix metalloproteinase-1 production
-
-
?
annexin A2 + H2O
?
-
stimulation of macrophages with plasmin leads to cleavage of ca. 6% of annexin A2 yielding a proteolytic fragment of ca. 33 kDa
-
-
?
beta-casein + H2O
?
-
-
-
-
?
beta-casein + H2O
?
-
hydrolysis is highly dependent on photooxidation state of substrate
-
-
?
beta-casein + H2O
?
-
-
-
-
?
Boc-Val-Leu-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
?
Boc-Val-Leu-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
?
Boc-Val-Leu-Lys-4-methylcoumaryl-7-amide + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
casein + H2O
?
-
-
-
-
?
casein + H2O
?
-
acid casein
-
-
?
chromogranin A + H2O
hCgA-(360-373) + ?
-
-
-
?
chromogranin A + H2O
hCgA-(360-373) + ?
-
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 C3b + H2O
?
-
the enzyme inactivates the C3b molecule for complement C3b amplification
-
-
?
complement component C3b + H2O
?
-
cleavage by plasmin produces bands of 46000 Da, 40000 Da, 30000 Da and 17000 Da
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
i.e. S-2251
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
i.e. S2251
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
chromogenic substrate S2251
-
-
?
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
-
-
-
?
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
-
-
-
?
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
-
-
-
?
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
-
hydrolysis by the plasmin-staphylokinase complex is twofold lower than in the case of the plasmin(ogen)-streptokinase complex
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
-
-
-
-
?
factor VIII + H2O
?
-
cleaves the heavy chain of factor VIII into two terminal products, A137336 and A2 subunits, by limited proteolysis at Lys36, Arg336, Arg372, and Arg740. The 80-kDa light chain is converted into a 67-kDa subunit by cleavage at Arg1689 and Arg1721
-
-
?
factor VIII + H2O
?
-
plasmin catalyzes activation or inactivation of factor VIII. The A2 domain of factor VIII, in particular residue Arg484, contributes to a unique plasmin-interactive site within the heavy chain that promotes plasmin docking during cofactor inactivation cleavage of the heavy chain
-
-
?
Fibrin + H2O
?
-
-
-
-
?
Fibrin + H2O
?
-
the activation of plasminogen in blood plasma is the central event that results in the dissolution of the fibrin clot by proteolysis
-
-
?
Fibrin + H2O
?
-
fibrin is formed from fibrinogen by thrombin, EC 3.4.21.5
-
-
?
Fibrin + H2O
?
-
fibrin is broken down through the liberation of plasmin from plasminogen via cleavage by either tissue plasminogen activator and/or urokinase plasminogen activator
-
-
?
fibrin + H2O
soluble fibrin fragments
-
-
-
-
?
fibrin + H2O
soluble fibrin fragments
-
-
-
?
fibrin + H2O
soluble fibrin fragments
cleavage of the Lys583-Met584 peptide bond in the Aalpha chain, followed by the cleavage of the peptide bonds Lys206-Met207 and Lys230-Ala231, also in the Aalpha chain, thus releasing a C-terminal 40-kDa fragment and generating fragment X possessing 260 kDa. Cleavage of fragment X in all three chains results in one fragment Y (160 kDa) and one fragment D (100 kDa), and further cleavage of fragment Y produces a second fragment D and fragment E (60 kDa)
-
-
?
Fibrinogen + H2O
?
-
-
-
-
?
Fibrinogen + H2O
?
-
the fibrinogen alpha-chain is degraded in low-molecular-mass fragments of approximately 63000-60000 Da
-
-
?
hemofiltrate CC chemokine 1 + H2O
[9-74] processed variant of hemofiltrate CC chemokine 1 + ?
-
-
further degradation of the active product
?
hemofiltrate CC chemokine 1 + H2O
[9-74] processed variant of hemofiltrate CC chemokine 1 + ?
-
urokinase plasminogen activator and plasmin efficiently convert hemofiltrate CC chemokine 1 into its active [9-74] processed variant
-
?
osteopontin + H2O
?
-
osteopontin is cleaved at multiple sites close to its integrin-binding motifs in milk and is a substrate for plasmin and cathepsin D
-
-
?
osteopontin + H2O
?
-
osteopontin, purified from human milk, is cleaved at multiple sites close to its integrin-binding motifs, e.g. cleavage at Arg152-Ser153, detailed overview
-
-
?
plasminogen + H2O
?
-
-
-
-
?
plasminogen + H2O
?
-
-
-
-
?
platelet-derived growth factor-C + H2O
?
-
plasmin is the major protease responsible for processing platelet-derived growth factor-C in patients undergoing retinal surgery. Plasmin is vastly more potent (192times faster) than tissue plasminogen activator in processing the substrate
-
-
?
platelet-derived growth factor-C + H2O
?
-
plasmin is the major protease responsible for processing platelet-derived growth factor-C in rabbits with proliferative vitreoretinopathy
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
-
-
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
-
-
-
?
Tosyl-Arg methyl ester + H2O
?
-
p-tosyl-Arg methyl ester
-
-
?
Tosyl-Arg methyl ester + H2O
?
-
-
-
-
?
tosyl-Gly-Pro-Lys-4-nitroanilide + H2O
tosyl-Gly-Pro-Lys + 4-nitroaniline
-
-
-
?
tosyl-Gly-Pro-Lys-4-nitroanilide + H2O
tosyl-Gly-Pro-Lys + 4-nitroaniline
-
-
-
-
?
vascular endothelial growth factor + H2O
?
-
cleavage site: Arg110-/-Ala111. The mutant vascular endothelial growth factors R110A, R110Q and A111P are resistant to cleavage
-
?
vascular endothelial growth factor + H2O
?
-
in non-healing wounds plasmin cleaves and inactivates vascular endothelial growth factor VEGF165
-
?
additional information
?
-
-
complexes of streptokinase with human plasminogen can hydrolytically activate other plasminogen molecules to plasmin, which then dissolve blood clots
-
-
?
additional information
?
-
-
the plasminogen activation system is mostly recognized for its fibrinolytic activity but is also upregulated in chronic inflammatory diseases, including atherosclerosis and arthritis. Plasmin is a potent activator of human monocytes and a number of other cells. In monocytes plasmin elicits full-blown proinflammatory activation encompassing lipid mediator release, chemotaxis and induction of cytokines and other proinflammatory genes. Cell activation is dependent on the binding of the plasmin molecule via its lysine binding sites as well as on the intact catalytic center of plasmin, indicating proteolytic activation. Cell activation occurs through a yet unidentified receptor which is specific for plasmin and that, at least in monocytes, is not activated by other proteases, such as factor Va and Xa, the serine proteases thrombin, alpha-chymotrypsin, human neutrophil elastase or cathepsin G
-
?
additional information
?
-
-
plasmin does not induce phosphorylation of JAK2 or JAK3. Does not activate SAP/JNK. Does not trigger activation and nuclear translocation ofSTAT1, STAT5A, or STAT5B
-
-
?
additional information
?
-
-
plasmin is 3-4fold less efficient in processing of the chromogranin A-Pro370Leu variant as compared to wild-type and the other varinats due to less efficient cleavage between Arg373-Arg374
-
-
?
additional information
?
-
-
plasmin triggeres phosphorylation of ERK1/2 in a concentration-dependent manner, but not of Akt
-
-
?
additional information
?
-
-
addition of plasmin to fibroblast-like cells from dental pulp induces an increase in the intracellular Ca2+ concentration, which may be inhibited by inhibition of receptor PAR-1. Plasmin stimulates the expression of interleukin-8 mRNA and prostaglandin E2 release
-
-
?
additional information
?
-
-
both plasmin and thrombin increase cell surface tissue factor activity in human pleural mesothelial cells by 3- to 4fold. Plasmin-induced tissue factor activity is not dependent on the de novo synthesis of tissue factor. In HUVEC, plasmin has a minimal effect on unperturbed HUVEC whereas it markedly increases tissue factor activity of activated HUVEC. Plasmin treatment neither affects anionic phospholipid levels at the cell surface nor releases protein disulfide isomerase
-
-
?
additional information
?
-
-
intravitreal plasmin injection increases the rate of vitreous removal in rabbits
-
-
?
additional information
?
-
-
plasmin can differentially modulate platelet aggregation in response to intrinsic heterogeneities within the insulin-like growth factor/insulin-like growth factor binding protein complexes
-
-
?
additional information
?
-
-
adherence of plasmin-coated encapsulated or unencapsulated pneumococci induces sporadic disruption of EaHy or A549 monolayer cell junctions
-
-
?
additional information
?
-
-
protein context, as well as the identity of amino acids at protease cleavage sites, dictate protease specificity
-
-
?
additional information
?
-
-
plasmin selectively cleaves arginyl-X and lysyl-X peptide bonds in many target proteins
-
-
?
additional information
?
-
rather broad specificity of plasmin in vivo catalyzing the inactivation and degradation of matrix proteins such as collagens, fibronectin, and laminins, and components of the blood coagulation cascade such as coagulation factor FVa, von Willebrand factor, and thrombospondin
-
-
?
additional information
?
-
-
subsite interactions of plasmin with substrates and inhibitors through computational docking analysis using the structure with PDB ID 1BML for plasmin in complex with streptokinase and no ligand molecules, molecular dynamic simulation of plasmin, overview. D/L-Ile-Phe-Lys substrate-binding modes
-
-
?
additional information
?
-
-
plasmin, possessing various substrate binding sites, shows substrate binding site cooperativity, molecular modeling of the plasmin-Ac-RM(O2)YR-H complex
-
-
?
additional information
?
-
-
staphylokinase forms a 1:1 stoichiometric complex with human plasmin and switches its substrate specificity to generate a plasminogen activator complex
-
-
?
additional information
?
-
-
substrate competition with urokinase-type plasminogen activator and bistability, overview
-
-
?
additional information
?
-
-
plasmin can activate collagenases
-
-
?
additional information
?
-
-
plasmin may serve as an endogenous PAR1 activator that can increase Ca2+ concentration, in astrocytes and potentiate N-methyl-D-aspartate receptor synaptic currents in CA1 pyramidal neurons
-
-
?
additional information
?
-
-
role for plasmin in augmenting hematopoietic progenitor cell mobilization in response to granulocyte colony-stimulating factor
-
-
?
additional information
?
-
-
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
-
-
?
additional information
?
-
-
potentiates TLR2 and TLR4 signalling in RAW264.7 macrophages. Enhances endogenous production of TNFalpha and activation of an NF-kappaB reporter plasmid
-
-
?
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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
-
-
(12S,15S)-12-(1H-indol-3-ylmethyl)-10,13-dioxo-N-(4-oxotetrahydrofuran-3-yl)-2-oxa-11,14-diazabicyclo[15.2.2]henicosa-1(19),17,20-triene-15-carboxamide
-
-
(4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-phenyl-propionylamino]-phenyl)-acetic acid
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.63 mM
(9S,12S)-9-(1H-indol-3-ylmethyl)-7,10-dioxo-N-(4-oxotetrahydrofuran-3-yl)-2-oxa-8,11-diazabicyclo[12.2.2]octadeca-1(16),14,17-triene-12-carboxamide
-
-
(E)-5,5'-(but-2-ene-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4Hchromen-4-one
-
about 43% residual activity at 0.4 mM
2-(3-[3-[(6-amino-hexyl)-(2-benzyloxycarbonylamino-3-phenyl-propionyl)-amino]-2-oxo-cyclohexyl]-propionylamino)-3-(1H-indol-3-yl)-propionic acid methyl ester
-
IC50: 0.024 mM
2-[(4-Aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionic acid pyridin-2-ylmethyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0042 mM
2-[3-(3-[(6-amino-hexyl)-[2-benzyloxycarbonylamino-3-(1H-indol-3-yl)-propionyl]-amino]-2-oxo-cyclohexyl)-propionylamino]-3-(1H-indol-3-yl)-propionic acid methyl ester
-
IC50: 0.02 mM
3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)heptyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one
-
about 1% residual activity at 0.4 mM
3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)octyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one
-
about 2% residual activity at 0.4 mM
4-(2-aminoethyl)benzenesulfonyl fluoride
-
-
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.024 mM, IC50 in reaction with fibrin is 0.0039 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid hexyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.018 mM, IC50 in reaction with fibrin is 0.0043 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid methyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0009 mM, IC50 in reaction with fibrin is 0.0061 mM
4-({2-(6-amino-hexanoylamino)-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid octyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is above 0.1 mM, IC50 in reaction with fibrin is 0.005 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid heptyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0014 mM, IC50 in reaction with fibrin is 0.00042 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid hexyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0015 mM, IC50 in reaction with fibrin is 0.0004 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid methyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.001 mM, IC50 in reaction with fibrin is 0.00078 mM
4-({2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-3-[4-(2-bromo-benzyloxycarbonyloxy)-phenyl]-propionylamino}-methyl)-cyclohexanecarboxylic acid octyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0025 mM, IC50 in reaction with fibrin is 0.00056 mM
4-amidinophenyl methane-sulfonyl fluoride
4-aminobenzamidine
-
competitive inhibition
4-aminomethylbenzamidine
-
competitive inhibition
4-carboxybenzamidine
-
competitive inhibition
479-504 peptide of factor VIII
-
blocks A2 subunit binding to Ah-plasmin by ca. 50% in a dose-dependent manner
-
484-509 peptide of factor VIII
-
blocks A2 subunit binding to Ah-plasmin by ca. 50% in a dose-dependent manner
-
489-514 peptide of factor VIII
-
weakly inhibits binding of the A2 subunit and plasmin with ca. 80% residual binding at the highest concentration (0.8 mM) of peptide
-
5,5'-(butane-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4H-chromen-4-one
-
about 42% residual activity at 0.4 mM
A2 subunit of factor VIII
-
plasmin-catalyzed activation of factor VIII is significantly inhibited by the addition of isolated A2 subunit of factor VIII in a dose-dependent manner
-
actin
-
actin inhibition of the fibrinolytic activity of plasmin is due to its competition with fibrin for the lysine binding sites of the enzyme
Aedes aegypti trypsin inhibitor
-
-
AG490
-
JAK inhibitor, inhibits JAK1 but does not inhibit TYK2 phosphorylation by plasmin. Impairs plasmin-mediated phosphorylation of ERK1/2, Akt1, and the subsequent phosphorylation of IkappaBalpha, but not that of p38 MAPK. Inhibits plasmin-induced TNF-alpha release by 63% and IL-6 release by 76%
Ah-plasmin
-
immobilized Ah-plasmin inhibits the A2 binding to Ah-plasmin by ca. 80% in a dose-dependent manner
-
AKbetaBA
-
inhibits plasmin-induced TNF-alpha release by 70%. Inhibits plasmin-induced activation of NF-kappaB by 66%
alpha(2)-plasmin inhibitor
-
alpha-antiplasmin
potent inhibitor
-
alpha-lactalbumin
-
shows a strong correlation with plasmin activity and may have inhibitory activity against plasmin
-
alpha1-protease inhibitor
-
plasmin bound to fibrin is completely protected
-
alpha2-Plasmin inhibitor
-
kringle domains K2, K3, and K5 are involved in the modulation of Plm activity
-
aminomethyl cyclohexane carboxylic acid
-
-
amyloid precursor-like protein 2
-
-
annexin II tetramer
-
promotes plasmin inactivation by stimulating the autoproteolytic digestion of plasmin heavy and light chains, also stimulates formation of plasmin. annexin II tetramer may function to provide the cell surface with a transient pulse of plasmin activity
-
antiplasmin
-
the inhibition of plasmin by antiplasmin can be reduced by high molecular weight fibrin degradation products with carboxy-terminal lysine residues
-
arsenic acid
-
organometallic complexes composed of humic acid and arsenic acid show enhanced inhibition of plasmin activity as compared with either arsenic or humic acid alone
beta-Lactoglobulin
-
native and denatured beta-lactoglobulin inhibits activity with D-Val-L-Leu-L-Lys-p-nitroanilide and casein
-
bikazin salivary inhibitor
-
-
Blood serum
-
bovine or ovine blood serum do not affect hydrolysis of caseins in milk by plasmin. Equine and particularly porcine serum strongly inhibit casein hydrolysis. Heated serum (70°C for 5 min) from any of the species does not influence plasmin-induced hydrolysis of caseins. Bovine or ovine serum (2%) have no effect on plasmin activity when assayed on N-Suc-L-Ala-L-Phe-L-Lys-7-amido-4-methyl-coumarin in milk. 2.0% porcine serum reduces plasmin activity on this peptide by ca. 40%
-
C1 inhibitor
-
the C1-inhibitor in its native state inhibits plasmin without significant degradation. If the C1-inhibitor is in a denatured polymeric state as can easily occur during storage, or as produced by heating of the native protein, it will be extensively degraded by plasmin
-
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0062 mM, IC50 in reaction with fibrin is 0.0012 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-heptylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.011 mM, IC50 in reaction with fibrin is 0.0033 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-hexylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.013 mM, IC50 in reaction with fibrin is 0.0027 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-nonylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0083 mM, IC50 in reaction with fibrin is 0.0013 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-octylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.007 mM, IC50 in reaction with fibrin is 0.0018 mM
Carbonic acid 4-[(S)-2-(6-amino-hexanoylamino)-2-pentylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.01 mM, IC50 in reaction with fibrin is 0.0013 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.085 mM, IC50 in reaction with fibrin is 0.019 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-butyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.009 mM, IC50 in reaction with fibrin is 0.0023 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-hexyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.006 mM, IC50 in reaction with fibrin is 0.0035 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-(4-pentyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.009 mM, IC50 in reaction with fibrin is 0.0047 mM
carbonic acid 4-[2-(6-amino-hexanoylamino)-2-propylcarbamoyl-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0092 mM, IC50 in reaction with fibrin is 0.002 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.013 mM, IC50 in reaction with fibrin is 0.0017 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(3-methyl-butylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00046 mM, IC50 in reaction with fibrin is 0.000056 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-butyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00079 mM, IC50 in reaction with fibrin is 0.00009 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-ethyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00063 mM, IC50 in reaction with fibrin is 0.000098 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-hexyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00049 mM, IC50 in reaction with fibrin is 0.00024 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-methoxymethyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00023 mM, IC50 in reaction with fibrin is mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(4-pentyl-phenylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00057 mM, IC50 in reaction with fibrin is 0.00007 mM
carbonic acid 4-[2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-(pyridin-4-ylcarbamoyl)-ethyl]-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00098 mM, IC50 in reaction with fibrin is 0.00017 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-heptylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.00043 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-hexylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0012 mM, IC50 in reaction with fibrin is 0.00038 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-nonylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
potent and selective inhibitor for plasmin, IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0005 mM, IC50 in reaction with fibrin is 0.0001 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-pentylcarbamoyl-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.011 mM, IC50 in reaction with fibrin is 0.0001 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[(pyridin-2-ylmethyl)-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0015 mM, IC50 in reaction with fibrin is 0.00052 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[(pyridin-4-ylmethyl)-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is0.0053 mM, IC50 in reaction with fibrin is 0.0014 mM
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-[benzyl-carbamoyl]-ethyl}-phenyl ester 2-bromo-benzyl ester
-
IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.0011 mM, IC50 in reaction with fibrin is 0.0003 mM
chicken liver trypsin inhibitor
-
-
Cholesterol sulfate
-
reduces plasmin activity in a dose-dependent manner
cis-parinaric acid
-
more than 60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
CO
-
CO elicits hypofibrinolysis by enhancing alpha2-antiplasmin activity and decreasing plasmin activity
CU-2010
potent inhibitpr
-
D-Leu-Lys-benzylamide
-
weak inhibitor of amidolytic activity
D-Phe-Lys-benzylamide
-
inhibition of fibrinolytic activity, no inhibition of amidolytic activity
D-Val-Phe-Lys-chloromethyl ketone
-
inhibits the ability of plasmin to potentiate lipopolysaccharide signalling. Significantly inhibits the generation of TNFalpha from untransfected RAW cells after plasmin pretreatment and stimulated with LPS
diisopropyl fluorophosphate
-
does not block binding of hepatocytes from mice to immobilized plasmin, but blocks active site of plasmin and its ability to phosphorylate ERK1/2
discreplasminin
-
isolated from Tityus discrepans scorpion venom. Peptide with a relative molecular weight of less than 6000 Da and a pI value of 8.0. Discreplasminin strongly inhibits plasmin and moderately inhibits tissue plasminogen activator
-
disodium 2-methoxy-4-[(1E)-3-[4-methyl-2-(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 73% residual activity at 0.4 mM
disodium 2-methoxy-6-[(1E)-3-oxo-3-[2-(sulfonatooxy)phenyl]prop-1-en-1-yl]phenyl sulfate
-
about 40% residual activity at 0.4 mM
disodium 3,5-dimethoxy-2-[(2E)-3-[3-methoxy-4-(sulfonatooxy)phenyl]prop-2-enoyl]phenyl sulfate
-
about 40% residual activity at 0.4 mM
disodium 3,5-dimethoxy-2-[(2E)-3-[4-methoxy-3-(sulfonatooxy)phenyl]prop-2-enoyl]phenyl sulfate
-
about 75% residual activity at 0.4 mM
disodium 3-(4-oxo-3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 40% residual activity at 0.4 mM
disodium 3-(acetyloxy)-5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 84% residual activity at 0.4 mM
disodium 3-[4-oxo-3-[3-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]propyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 35% residual activity at 0.4 mM
disodium 4-(4-oxo-3,4-dihydroquinazolin-2-yl)benzene-1,3-diyl disulfate
-
about 77% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[5-[5-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]pentyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 25% residual activity at 0.4 mM; about 35% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 5% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[[1-(12-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]dodecyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 2% residual activity at 0.4 mM; about 30% residual activity at 0.4 mM; about 40% residual activity at 0.4 mM
disodium 4-(4-oxo-3-[[1-(7-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]heptyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 30% residual activity at 0.4 mM
disodium 4-[(2E)-3-(2-methoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate
-
about 39% residual activity at 0.4 mM
disodium 4-[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate
-
about 31% residual activity at 0.4 mM
disodium 4-[4-oxo-3-[11-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]undecyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 3% residual activity at 0.4 mM
disodium 4-[4-oxo-3-[8-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]octyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 7% residual activity at 0.4 mM
disodium 4-[4-oxo-3-[9-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]nonyl]quinazolin-2(4H)-yl]phenyl sulfate
-
about 7% residual activity at 0.4 mM
disodium 4-[4-oxo-6-(sulfonatooxy)-4H-chromen-2-yl]phenyl sulfate
-
about 85% residual activity at 0.4 mM
elaidic acid
-
60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
epsilon-aminocaproic acid
-
inhibits plasmin-induced phosphorylation of ERK1/2; lysine binding sites inhibitor, partially blocks binding of hepatocytes from mice to immobilized plasmin at 10 mM, but not at 0.01 mM
Fibrin
-
inhibits hydrolysis of D-Val-Leu-Lys-p-nitroanilide
fragment X
-
competitive inhibitor of plasmin chromogenic activity
-
histidine-rich glycoprotein
binds at sites of tissue injury and seems to act as a high-affinity receptor to immobilize plasminogen on cell surfaces
-
human aprotinin analogue
-
-
-
human plasma protein inhibitors
-
-
-
humic acid
-
0.02-0.48 mg/ml, up to 95% inhibition, natural and synthetic. Organometallic complexes composed of humic acid and arsenic acid show enhanced inhibition of plasmin activity as compared with either arsenic or humic acid alone
hydroxyethyl starch 130
-
plasma diluted with hydroxyethyl starch 130 has a significant more than 25% attenuation of plasmin-mediated decreases in the maximum rate of thrombus generation and total thrombus generation compared with 0.9% NaCl diluted and undiluted plasma. Enhances fibrinolysis by diminishing alpha2-antiplasmin-plasmin interactions
-
Kunitz-type inhibitor 2
-
-
L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
LEKTI
-
potent noncompetitive inhibitor, recombinant LEKTI is purified using a baculovirus/insect cell expression system
Leu-Lys-benzylamide
-
inhibition of fibrinolytic activity, no inhibition of amidolytic activity
Leucaena-type trypsin inhibitor
-
-
leupeptin
-
inhibits the ability of plasmin to potentiate lipopolysaccharide signalling
Lima bean trypsin inhibitor
-
-
-
Lys-Met(sulfone)-Tyr-Arg
-
shows 25fold selectivity for plasmin over plasma kallikrein
mAb413
-
antibody of A2 subunit, that blocks plasmin-catalyzed factor VIII heavy chain cleavage at Arg336 and Arg372, but not at Arg740. This antibody does not affect plasmin-catalyzed cleavage of the light chain
-
MG-132
-
prevents facilitation of degradation of Bim(EL) by plasmin in hepatocytes from mice pretreated with cycloheximide
N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzyloxycarbonyl)-octylamide
-
potent and selective inhibitor for plasmin, IC50 in reaction with D-Val-Leu-Lys-4-nitroanilide is 0.00023 mM, IC50 in reaction with fibrin is 0.0008 mM
N-oleoyl heparin
-
noncompetitive inhibition
-
N-[(1S)-5-amino-1-cyanopentyl]-3-([3-[1-(4-fluorobenzyl)-1H-indol-3-yl]propanoyl]amino)-4-(pyridin-4-ylmethoxy)benzamide
-
molecular modeling
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-1-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-3-[(naphthalen-2-ylacetyl)amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-3-[[(4-fluorophenyl)acetyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-3-[[3-(1H-indol-3-yl)propanoyl]amino]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(1S)-5-amino-1-cyanopentyl]-4-(pyridin-4-ylmethoxy)benzamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(1-glycyl-4-oxopyrrolidin-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclohexyl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclopentyl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobenzyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-aminobutyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(4-oxotetrahydrofuran-3-yl)-L-tryptophanamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(5-aminopentyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(1,1-dioxido-4-oxotetrahydrothiophen-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(6-aminohexyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(7-aminoheptyl)-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-[(trans-4-aminocyclohexyl)methyl]-N-(4-oxotetrahydrofuran-3-yl)-L-phenylalaninamide
-
-
Nalpha-[[trans-4-(aminomethyl)cyclohexyl]carbonyl]-N-hexyl-O-(pyridin-4-ylmethyl)-L-tyrosinamide
-
binding mode
Nomega-nitro-L-arginine methyl ester
-
almost completely abolishes plasmin-induced relaxation
octasodium [(ethane-1,2-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-4,1,2-triyl] tetrasulfate
-
about 16% residual activity at 0.4 mM; about 18% residual activity at 0.4 mM; about 65% residual activity at 0.4 mM
octasodium [(propane-1,3-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-1,2,4-triyl] tetrasulfate
-
about 30% residual activity at 0.4 mM
oleic acid
-
59% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
ONO-3307
i.e. 4-sulfamoyl phenyl-4-guanidinobenzoate methanesulfonate
Pancreatic trypsin inhibitor
-
PD98059
-
MEK inhibitor, completely abolishes plasmin-induced phosphorylation of ERK1/2 at 0.05 mM
Pentamidine
-
competitive inhibition
pentasodium (2R)-2-[3,4-bis(sulfonatooxy)phenyl]-3,4-dihydro-2H-1-benzopyran-3,6,7-triyl trisulfate
-
about 32% residual activity at 0.4 mM
pentasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-5-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methoxy]-4H-1-benzopyran-3,7-diyl disulfate
-
about 5% residual activity at 0.4 mM
pentasodium 2-[3-[2,5-bis(sulfonatooxy)phenyl]propanoyl]-5,8-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 73% residual activity at 0.4 mM
pentasodium 2-[3-[2,5-bis(sulfonatooxy)phenyl]propanoyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 60% residual activity at 0.4 mM
pentasodium 2-[4-[2,5-bis(sulfonatooxy)phenyl]butanoyl]-5,8-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 78% residual activity at 0.4 mM
pentasodium 2-[4-[2,5-bis(sulfonatooxy)phenyl]butanoyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 80% residual activity at 0.4 mM
pentasodium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 75% residual activity at 0.4 mM
pentasopentasodium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylatedium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
-
about 70% residual activity at 0.4 mM
peptide GHRPYam
-
delays appearance of plasmin activity
peroxynitrite
-
50% inhibition at 280 microM and an enzyme concentration of 10 microM
Phe-Lys-benzylamide
-
inhibition of fibrinolytic activity, no inhibition of amidolytic activity
plasminogen activator inhibitor 1
-
-
plasminogen activator inhibitor I
-
plasminogen activator inhibitor II
-
plasminogen activator inhibitor-type 1
-
totally blocks plasmin activity and degradation of casein
-
plasminogen activator inhibitors 1
-
-
plasminogen activator inhibitors 2
-
-
Protein C inhibitor
-
from Bos taurus
-
R484A mutant of A2
-
subunit of factor VIII, possessing ca. 250fold reduced affinity for plasmin, weakly inhibits factor VIIIa inactivation by ca. 20%
-
recombinant aprotinin
-
-
-
RG1192
-
dextran containing carboxymethylsulfate as well as benzylamide groups. Lysine-binding site domain of plasmin is the RG1192 binding site. In addition RG1192 blocks the generation of plasmin from Glu-plasminogen and inhibits the plasmin-mediated proteolysis of fibronectin and laminin
-
SB203580
-
inhibits plasmin-induced TNF-alpha release by 75% and IL-6 release by 79%
serpinb2
-
steroid-treated ovariectomized mice deficient in tissue inhibitor of metalloprotease-1 and exposed to estrogen show a significant increase in plasmin activity. Increase is probably due to reduced expression of plasmin inhibitors serpinb7 and serpinb2
-
serpinb7
-
steroid-treated ovariectomized mice deficient in tissue inhibitor of metalloprotease-1 and exposed to estrogen show a significant increase in plasmin activity. Increase is probably due to reduced expression of plasmin inhibitors serpinb7 and serpinb2. Serpinb7 is localized to luminal and glandular epithelial cells of the uterus. Expression of serpinb7 is decreased by estrogen and shows an inverse relationship with plasmin activity
-
sodium 2,6-diformyl-4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 93% residual activity at 0.4 mM
sodium 3-(3-[[1-(4-[2-[3-(acetyloxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate
-
about 55% residual activity at 0.4 mM
Soybean trypsin inhibitor
-
sucrose octasulfate
-
about 99% residual activity at 0.4 mM
sulfated polyvinylalcohol-acrylate copolymers
-
both the amidolytic and fibrinolytic activities are inhibited
-
TdPI tryptase inhibitor
-
-
tert-butyl 3-(3-[[5-[[(1S)-5-amino-1-cyanopentyl]carbamoyl]-2-(pyridin-4-ylmethoxy)phenyl]amino]-3-oxopropyl)-1H-indole-1-carboxylate
-
-
tetrasodium 2-[2,4-bis(sulfonatooxy)phenyl]-5-hydroxy-4-oxo-4H-chromene-3,7-diyl disulfate
-
about 45% residual activity at 0.4 mM
tetrasodium 2-[2-[6,7-bis(sulfonatooxy)-3,4-dihydroisoquinolin-2(1H)-yl]-2-oxoethyl]-1,4-phenylene disulfate
-
about 60% residual activity at 0.4 mM
tetrasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-4H-chromene-3,7-diyl disulfate
-
about 99% residual activity at 0.4 mM
tetrasodium 2-[4-[5,6-bis(sulfonatooxy)-3,4-dihydroisoquinolin-2(1H)-yl]-4-oxobutyl]-1,4-phenylene disulfate
-
about 48% residual activity at 0.4 mM
tetrasodium 4-[5-hydroxy-4-oxo-3,7-bis(sulfonatooxy)-4H-chromen-2-yl]benzene-1,2-diyl disulfate
-
about 93% residual activity at 0.4 mM
tetrasodium 5-methoxy-2-[3-[[1-(4-[2-[3-methoxy-4-(sulfonatooxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4-oxo-4H-1-benzopyran-3,7-diyl disulfate
-
about 3% residual activity at 0.4 mM; about 7% residual activity at 0.4 mM; about 8% residual activity at 0.4 mM
tetrasodium 5-methoxy-4-oxo-2-[3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4H-1-benzopyran-3,7-diyl disulfate
-
about 20% residual activity at 0.4 mM
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
-
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
-
-
trans-parinaric acid
-
60% inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
transforming growth factor-b1
-
reduces plasminogen conversion to active plasmin in wild type tendon cells
-
trisodium 2-[(1E)-3-[2,4-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 42% residual activity at 0.4 mM
trisodium 4-oxo-2-[3-(sulfonatooxy)phenyl]-4H-chromene-3,7-diyl disulfate
-
about 82% residual activity at 0.4 mM
trisodium 4-[(1E)-3-[2,4-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 58% residual activity at 0.4 mM
trisodium 4-[(1E)-3-[2,5-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]-2-methoxyphenyl sulfate
-
about 90% residual activity at 0.4 mM
trisodium 4-[(1E)-3-[2,5-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate
-
about 51% residual activity at 0.4 mM
trisodium 5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)-1,3-phenylene disulfate
-
about 45% residual activity at 0.4 mM
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
4-amidinophenyl methane-sulfonyl fluoride
-
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
6-aminohexanoic acid
-
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
-
noncompetitive
6-aminohexanoic acid
-
the heavy chain plays an important role in the inhibition of the enzyme by 6-aminohexanoate
6-aminohexanoic acid
-
weak, competitive
alpha(2)-plasmin inhibitor
-
blocks plasmin activity
-
alpha(2)-plasmin inhibitor
-
blocks plasmin activity
-
alpha2-antiplasmin
-
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
the main physiological inhibitor and a serpin
-
alpha2-antiplasmin
-
inhibits proteolysis of rADAMTS13
-
alpha2-antiplasmin
-
contributes to the inactivation of plasmin activity
-
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
-
alpha2-Macroglobulin
-
similar inhibition 0f native enzyme and deletion mutant lacking the middle portion of the molecule
-
alpha2-Macroglobulin
general protease inhibitor
-
alpha2-Macroglobulin
-
plasmin bound to fibrin is completely protected
-
Aprotinin
-
complete inhibition of pro-matrix metalloproteinase-3 activation at 0.05 mM
Aprotinin
-
inhibits plasmin-induced phosphorylation of ERK1/2
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
benzamidine
-
competitive inhibition
benzamidine
-
competitive
fibrinogen
-
competitive inhibitor of plasmin chromogenic activity
-
fibrinogen
-
inhibits hydrolysis of D-Val-Leu-Lys-p-nitroanilide. 6-aminohexanoic acid abolishes inhibition
-
neuroserpin
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
-
neuroserpin
-
an axonally secreted serine proteinase inhibitor
-
Pancreatic trypsin inhibitor
-
-
-
Pancreatic trypsin inhibitor
-
-
-
plasminogen activator inhibitor I
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
plasminogen activator inhibitor I
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
plasminogen activator inhibitor II
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
plasminogen activator inhibitor II
-
inhibits plasminogen activation to plasmin by urokinase-type plasminogen activator
-
Soybean trypsin inhibitor
-
-
-
Soybean trypsin inhibitor
-
-
-
textilinin-1
-
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
-
Tranexamic acid
-
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
Tranexamic acid
-
substantially abrogates the relaxing effect of plasmin
additional information
-
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
-
no inhibition by protein C inhibitor from Bos taurus
-
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
-
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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
-
-
0.075
(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
Homo sapiens
-
at pH 7.4 and 37°C
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
0.056
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
Homo sapiens
-
at pH 7.4 and 37°C
0.045
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
Homo sapiens
-
at pH 7.4 and 37°C
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
0.076
5,5'-(butane-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4H-chromen-4-one
Homo sapiens
-
at pH 7.4 and 37°C
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
Homo sapiens
-
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
0.0001
carbonic acid 4-{2-[(4-aminomethyl-cyclohexanecarbonyl)-amino]-2-pentylcarbamoyl-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 0.0001 mM
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
0.4
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
Homo sapiens
-
at pH 7.4 and 37°C
1
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
Homo sapiens
-
at pH 7.4 and 37°C
0.4
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
Homo sapiens
-
at pH 7.4 and 37°C
0.125 - 0.239
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
0.098
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
Homo sapiens
-
at pH 7.4 and 37°C
0.089 - 0.621
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
0.161
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
Homo sapiens
-
at pH 7.4 and 37°C
0.111
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
Homo sapiens
-
at pH 7.4 and 37°C
0.183
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
Homo sapiens
-
at pH 7.4 and 37°C
0.137
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
Homo sapiens
-
at pH 7.4 and 37°C
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
0.000016
N-oleoyl heparin
Homo sapiens
-
at pH 7.4 and 37°C
-
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
synthetic construct
-
-
1
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-(2-oxocyclopentyl)-L-phenylalaninamide
synthetic construct
-
-
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
0.185 - 2.83
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
0.4
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
Homo sapiens
-
at pH 7.4 and 37°C
0.13
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
Homo sapiens
-
at pH 7.4 and 37°C
0.63
PKSI-527
Homo sapiens
pH and temperature not specified in the publication
0.00037 - 0.00175
PSI-112
0.642
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
Homo sapiens
-
at pH 7.4 and 37°C
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
0.128 - 0.22
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
0.149
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
Homo sapiens
-
at pH 7.4 and 37°C
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
0.08679
Tranexamic acid
Homo sapiens
-
wild type enzyme, pH and temperature not specified in the publication
0.00017 - 0.00115
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
0.084
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
Homo sapiens
-
at pH 7.4 and 37°C
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
0.125
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
Homo sapiens
-
at pH 7.4 and 37°C
0.239
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
Homo sapiens
-
at pH 7.4 and 37°C
0.089
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
Homo sapiens
-
at pH 7.4 and 37°C
0.277
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
Homo sapiens
-
at pH 7.4 and 37°C
0.621
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
Homo sapiens
-
at pH 7.4 and 37°C
0.185
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
Homo sapiens
-
at pH 7.4 and 37°C
0.209
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
Homo sapiens
-
at pH 7.4 and 37°C
2.83
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
Homo sapiens
-
at pH 7.4 and 37°C
0.00037
PSI-112
Homo sapiens
-
mutant enzyme K607A, pH and temperature not specified in the publication
0.00038
PSI-112
Homo sapiens
-
wild type enzyme, pH and temperature not specified in the publication
0.00148
PSI-112
Homo sapiens
-
mutant enzyme F587A, pH and temperature not specified in the publication
0.00175
PSI-112
Homo sapiens
-
mutant enzyme F587A/K607A, pH and temperature not specified in the publication
0.128
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
Homo sapiens
-
at pH 7.4 and 37°C
0.157
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
Homo sapiens
-
at pH 7.4 and 37°C
0.22
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
Homo sapiens
-
at pH 7.4 and 37°C
0.00017
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
Homo sapiens
-
mutant enzyme K607A, pH and temperature not specified in the publication
0.00024
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
Homo sapiens
-
wild type enzyme, pH and temperature not specified in the publication
0.0011
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
Homo sapiens
-
mutant enzyme F587A/K607A, pH and temperature not specified in the publication
0.00115
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
Homo sapiens
-
mutant enzyme F587A, pH and temperature not specified in the publication
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