Information on EC 3.4.21.73 - u-Plasminogen activator

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The expected taxonomic range for this enzyme is: Opisthokonta

EC NUMBER
COMMENTARY hide
3.4.21.73
-
RECOMMENDED NAME
GeneOntology No.
u-Plasminogen activator
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Specific cleavage of Arg-/-Val bond in plasminogen to form plasmin
show the reaction diagram
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-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
139639-24-0
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
Manually annotated by BRENDA team
Mus musculus C57BL/6J
C57BL/6J mice
-
-
Manually annotated by BRENDA team
Mus musculus E16-E18
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-
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
-
the enzyme belongs to the trypsin superfamily of enzymes
malfunction
metabolism
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
alpha6 integrin + H2O
?
show the reaction diagram
benzoyl-beta-Ala-Gly-Arg-4-nitroanilide + H2O
benzoyl-beta-Ala-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Benzyloxycarbonyl-Gly-Gly-Arg-amino-4-trifluoromethylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
-
casein + H2O
?
show the reaction diagram
-
-
-
-
?
Cellular receptor of urokinase-type plasminogen activator + H2O
?
show the reaction diagram
-
cleavage between domains 1 and 2 generating a cell-associated variant of the receptor of urokinase-type plasminogen activator without ligand-binding properties, uPA catalyzed cleavage does not require binding of the protease to the receptor through its epidermal growth factor-like receptor-binding domain, low-molecular weight uPA lacking this domain also cleaves the substrate
-
-
-
D-Glu-Gly-Arg-4-nitroanilide + H2O
D-Glu-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
a uPA substrate S-2444
-
-
?
D-Ile-Pro-Arg-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
D-Val-Leu-Lys-4-nitroanilide + H2O
D-Val-Leu-Lys + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
di-Glu-Pro-Arg-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
epithelial sodium channel gamma subunit + H2O
?
show the reaction diagram
-
of Xenopus laevis ocytes, activation by proteolytic cleavage at 177GR-/-KR180
-
-
?
GSGRSA + H2O
GSGR + Ser-Ala
show the reaction diagram
-
-
-
?
HYGRSA + H2O
HYGR + Ser-Ala
show the reaction diagram
-
-
-
?
Kininogen + H2O
Kinin
show the reaction diagram
-
-
-
-
L-diglutamyl-glycyl-L-arginine 4-nitroanilide + H2O
L-diglutamyl-glycyl-L-arginine + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-pyroGlu-Gly-L-Arg-4-nitroanilide + H2O
?
show the reaction diagram
L-pyroglutamyl-glycyl-L-arginine-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
?
PFGRSA + H2O
PFGR + Ser-Ala
show the reaction diagram
-
-
-
?
plasmin + H2O
?
show the reaction diagram
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-
-
-
?
plasminogen + H2O
?
show the reaction diagram
plasminogen + H2O
plasmin + ?
show the reaction diagram
pro-hepatic growth factor + H2O
mature hepatic growth factor + ?
show the reaction diagram
pyroGlu-Gly-Arg-4-nitroanilide + H2O
pyroGlu-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
i.e. S-2444, a chromogenic substrate
-
-
?
QRGRSA + H2O
QRGR + Ser-Ala
show the reaction diagram
-
-
-
?
S-2444 + H2O
?
show the reaction diagram
S2444 + H2O
?
show the reaction diagram
-
i.e. 5-oxo-L-Pro-Gly-L-Arg-p-nitroanilide
-
?
t-butyloxycarbonyl-valyl-leucyl-lysine-4-methylcoumaryl-7-amide + H2O
?
show the reaction diagram
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-
-
-
?
thrombin + H2O
?
show the reaction diagram
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-
-
-
?
urokinase plasminogen activator receptor + H2O
?
show the reaction diagram
YGAKAY + H2O
YGAK + Ala-Tyr
show the reaction diagram
-
-
-
?
Z-RRG-7-amido-4-methylcoumarin + H2O
Z-RRG + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
additional information
?
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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
alpha6 integrin + H2O
?
show the reaction diagram
-
alpha6 integrin is present on prostate carcinoma escaping the gland via nerves. Urokinase-dependent cleavage of the laminin binding domain from the prostate tumor cell surface
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-
?
plasminogen + H2O
?
show the reaction diagram
plasminogen + H2O
plasmin + ?
show the reaction diagram
pro-hepatic growth factor + H2O
mature hepatic growth factor + ?
show the reaction diagram
urokinase plasminogen activator receptor + H2O
?
show the reaction diagram
-
receptor cleavage by u-PA, u-PAR is susceptible to proteolysis by its cognate ligand and several other proteases, biological significance, overview
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-
?
additional information
?
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-[(N-benzylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
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1-[3'-([3,5-difluoro-6-[5-methyl-2-(1H-tetrazol-1-yl)phenoxy]pyridin-2-yl]oxy)biphenyl-3-yl]methanamine
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2-(1-hydroxynaphthalen-2-yl)-1-H-benzoimidazole-5-carboxamidine
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2-(2,6-dihydroxyphenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-3-bromo-5-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-3-bromophenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-3-fluorophenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-3-methoxyphenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-3-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
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-
2-(2-hydroxy-3-nitrophenyl)-1-H-benzoimidazole-5-carboxamidine
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-
2-(2-hydroxy-4-diethylaminophenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-4-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
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-
2-(2-hydroxy-5-bromophenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxy-5-chlorobiphenyl-3-yl)-1-H-benzoimidazole-5-carboxamidine
-
-
2-(2-hydroxy-5-fluorophenyl)-1-H-benzoimidazole-5-carboxamidine
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-
2-(2-hydroxy-5-methoxyphenyl)-1-H-benzoimidazole-5-carboxamidine
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-
2-(2-hydroxy-5-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
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-
2-(2-hydroxy-5-nitrophenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxybiphenyl-3-yl)-1-H-benzoimidazole-5-carboxamidine
-
-
2-(2-hydroxyphenyl)-1-H-benzoimidazole-5-carboxamidine
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2-(2-hydroxyphenyl)1H-benzoimidazole-5-carboxamidine
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2-(4-chloro-7-(2-cyano-6-methoxyphenyl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(4-chloro-7-(2-methoxyphenyl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(4-chloro-7-(3-methoxyphenyl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(7-(1,3-benzodioxol-5-yl)-4-chloroisoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(7-(1,3-benzodioxol-5-yl)isoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-(7-phenylisoquinolin-1-yl)guanidine
-
comparison of selectivity with t-plasminogen activator and plasmin
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
-
-
2-phenethyl-SO2-D-Ser-Ala-Arg-al
-
is an irreversible urokinase inhibitor, and an alkylating agent forming a covalent adduct with an active site of the enzyme
2-phenyl-1-H-benzoimidazole-5-carboxamidine
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-
2-[(6-[[3',5-bis(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)-5-hydroxybiphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-3-methylbenzoic acid
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-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
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-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(propan-2-yl)benzoic acid
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2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methoxybenzoic acid
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2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
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-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-nitrobenzoic acid
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-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-5-methylbenzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-6-methylbenzoic acid
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2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
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2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
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-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[[2-(dimethylamino)ethyl](methyl)amino]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
-
-
2-[(6-[[4'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
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-
2-[(6-[[4-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
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-
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[6-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[2-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
-
2-[2-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
-
2-[3-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)propyl]isothiourea hydrobromide
-
-
2-[3-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy]propyl)isothiourea hydrobromide
-
-
2-[[3,5-difluoro-6-([3'-[(methylamino)methyl]biphenyl-3-yl]oxy)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(methylamino)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(morpholin-4-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(piperazin-1-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-(dimethylamino)-3,5-difluoropyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
-
-
3,5 diamino-6-chloro-N-(diaminomethylene)pyrazinecarboximide
-
i.e. amiloride, selectively inhibits the enzyme, but not tissue plasminogen activator or other serine protease members of the trypsin superfamily
-
3-(1-carbamimidoylpiperidin-3-yl)-L-alanine
3-(1-carbamimidoylpiperidin-4-yl)-L-alanine
3-(2-bromoethoxy)-7-nitro-1H-isochromen-1-one
-
-
3-(3-bromopropoxy)-4-trifluoroacetyl-1H-isochromen-1-one
-
-
3-(3-bromopropoxy)-7-nitro-1H-isochromen-1-one
-
-
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)-5-methoxybenzoic acid
-
comparison of selectivity with t-plasminogen activator and plasmin
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
comparison of selectivity with t-plasminogen activator and plasmin
3-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
-
3-[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]propanoic acid
-
-
4'-(6-cyano-2-naphthamido)biphenyl-3-carboxylic acid
-
slight inhibition
4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxamide
-
slight inhibition
4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide
-
inhibitor with moderate clearance level, high volume of distribution, and long half-life of 7.5 hours. More than 50 fold selective for uPA over all but one of the enzymes tested. Selectivity against trypsin is only 3- to 4fold
4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
-
-
4-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
comparison of selectivity with t-plasminogen activator and plasmin
4-(dimethylamino)-2-[[6-([3'-[(dimethylamino)methyl]biphenyl-3-yl]oxy)-3,5-difluoropyridin-2-yl]oxy]benzoic acid
-
-
4-aminobenzamidine
-
competitive, no inhibition of the pro-uPA
4-chloro-3-alkoxyisocoumarin
-
competitive reversible inhibition
4-iodobenzo[b]thiophene-2-carboxamidine
-
APC-6860, competitive inhibition
4-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
-
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
-
-
6-(phenylcarbamoyl)-2-naphthoic acid
-
slight inhibition
6-amino-N-phenyl-2-naphthamide
-
slight inhibition
6-bromo-N-phenyl-2-naphthamide
-
slight inhibition
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
-
-
6-carbamimidoyl-N-phenyl-2-naphthamide
-
-
6-carbamimidoyl-N-phenyl-5,8-dihydronaphthalene-2-carboxamide
-
-
6-cyano-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
-
-
6-cyano-N-(3,5-dimethoxyphenyl)-2-naphthamide
-
-
6-cyano-N-phenylnaphthalene-2-carboxamide
-
slight inhibition
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
-
-
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
-
-
6-methoxy-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
-
-
6-methoxy-N-(3'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
-
-
6-methoxy-N-(3'-nitrobiphenyl-4-yl)-2-naphthamide
-
-
6-methoxy-N-(3'-nitrobiphenyl-4-yl)naphthalene-2-sulfonamide
-
-
6-methoxy-N-(4'-methoxybiphenyl-4-yl)-2-naphthamide
-
-
6-methoxy-N-(4'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
-
-
6-methoxy-N-phenyl-2-naphthamide
-
slight inhibition
7-amino-3-(2-bromoethoxy)-1H-isochromen-1-one
-
-
7-methoxy-8-[1-(methylsulfonyl)-1H-pyrazol-4-yl]naphthalene-2-carboximidamide
-
-
alpha-1-antitrypsin
-
-
-
alpha-1-Proteinase inhibitor
-
-
-
alpha-2-Macroglobulin
-
-
-
alpha-Benzylsulfonyl-p-aminophenylalanine
-
-
amiloride
Anti-uPA IgG
-
-
-
antibody DS2
-
isolation and affinity maturation of a fully human recombinant antibody, that is specific to the human uPA and capable of inhibiting its enzymatic activity with an IC50 value in the low nanomolar range, overview. Ability of the DS2 antibody to preferentially localize at the tumor site compared with healthy organs
-
antibody IgG(DS2)
-
-
-
antibody mU3
-
binding of mU3 to the 37- and 70-loops, the antibody stabilizes the active conformation of the enzyme, the N-terminus (Ile16) of the truncated enzyme muPA(16-243) is less exposed upon binding of mU3
-
antibody scFv(DS2)
-
-
-
antipain
-
-
antithrombin
-
-
-
Aprotinin
-
-
benzamidine
benzo[b]thiophene-2-carboxamidine
-
APC-7377
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
-
concanavalin A
-
-
-
D-Phe-Phe-ArgCH2Cl
-
-
D-Ser-Ala-Arg-NH-(CH2)5-NH2
-
competitive inhibition
D-Ser-Ala-Arg-NH-(CH2)7-NH2
-
-
D-Ser-Ala-Arg-NH-(CH2)8-NH2
-
-
D-Ser-Ala-Arg-NH-(CH2)9-NH2
-
-
di-(4-acetamidophenyl) 1-[(N-benzyloxycarbonyl-D-seryl)-Lalanyl]amino-2-[4-(guanidino)phenyl]-ethanephosphonate trifluoroacetate
-
-
diphenyl (N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(3-guanylpropyl)methanephosphonate
-
50% inhibition at 0.000061 mM
diphenyl (N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(4-guanylbutyl)methanephosphonate
-
50% inhibition at 0.00025 mM
diphenyl (N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(4-guanylphenyl)methanephosphonate
-
50% inhibition at 0.0016 mM
diphenyl 1-(N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-2-(4-guanylphenyl)ethanephosphonate
-
50% inhibition at 0.000057 mM
diphenyl 1-[(N-2-acetoadamantanyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-2-acetothiophenyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-benzenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-benzoyloxycarbonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-benzoylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-naphtalenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-o,o-dimethylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-o-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-bromobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-cyanobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-methoxybenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
-
-
diphenyl 1-[(N-p-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl 1-[(N2-thiophenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
-
-
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
-
ecotin
EDTA
-
inhibits binding of integrin alphanybeta3 to the enzyme
Endothelial cell/platelet type plasminogen activator inhibitor
-
-
-
enzyme-specific antibody
-
significant reduction of hair follicle keratinocyte proliferation
-
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
-
Fast-acting uPA inhibitor in plasma
-
-
-
Glu-Gly-Arg chloromethyl ketone
-
-
Glu-Gly-Arg-chloromethyl ketone
-
-
i-Boc-D-Ser-Ala-Arg-al
-
is an alkylating agent, and irreversibly inhibits urokinase by forming a covalent adduct with an active site of the enzyme
Leupeptin
-
-
Lima bean trypsin inhibitor
-
-
-
maspin
-
regulates uPA-dependent processes in vivo not involving its RCL sequence with Arg340, but is inable to directly inhibit uPA catalytic activity in vitro, binds the enzyme in both singlechain and double-chain forms, maspin is a member of the serpin family with a reactive center loop that is incompatible with proteinase inhibition by the serpin conformational change mechanism, overview
meloxicam
-
reduces enzyme secretion in chondral and synovial cultures downregulating the PA/plasmin system
methyl 4'-(2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-amino-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-bromo-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-chloro-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-cyano-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-methoxy-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-4-carboxylate
-
-
methyl 4'-(naphthalene-2-sulfonamido)biphenyl-3-carboxylate
-
-
methyl 4'-(naphthalene-2-sulfonamido)biphenyl-4-carboxylate
-
-
methyl 6-(3'-(methoxycarbonyl)biphenyl-4-ylcarbamoyl)-2-naphthoate
-
-
methyl 6-(phenylcarbamoyl)-2-naphthoate
-
slight inhibition
methylprednisolone
-
reduces enzyme secretion in chondral and synovial cultures downregulating the PA/plasmin system
mexiletine
-
IC50 value above 1 mM, crystallographic data
monoclonal antibody mU1
-
murine monoclonal antibody directed against murine uPA. mU1 blocks uPA-catalyzed plasminogen activation in vitro, as well as plasmin-mediated pro-uPA activation. Systemic administration of mU1 rescues mice treated with a uPA-activable anthrax protoxi and impairs uPA-mediated hepatic fibrinolysis in tissue-type plasminogen activator-deficient mice, resulting in a phenotype mimicking that of uPA/tPA double deficient mice
-
mupain-1
mupain-1-16
-
the inhibitor stabilizes the active conformation of the enzyme, the N-terminus (Ile16) of the truncated enzyme muPA(16-243) is less exposed upon binding of mupain-1-16
myristoylated PKI
-
mPLI, a protein kinase A inhibitor, complete inhibition
-
N-(2,4'-dimethoxybiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
-
N-(2,4-dimethoxybiphenyl-4-yl)-6-methoxy-2-naphthamide
-
slight inhibition
N-(3',4'-dimethoxybiphenyl-4-yl)-6-methoxy-2-naphthamide
-
-
N-(3',4'-dimethoxybiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
-
N-(3'-aminobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
-
N-(3'-chlorobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
slight inhibition
N-(3'-fluorobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
slight inhibition
N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
-
-
N-(3'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
-
-
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
-
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-(biphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
-
-
N-phenyl-2-naphthamide
-
slight inhibition
N-[(4-aminobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-methylbenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[(4-nitrobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N-[3-(2-bromoethoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
-
N-[3-(3-bromopropoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
competitive reversible inhibition mechanism, the bromine occupies the same position as positively charged arginino mimetic groups, molecular modeling
N-[4-(aminomethyl)phenyl]-6-carbamimidoyl-4-(pyrimidin-2-ylamino)naphthalene-2-carboxamide
-
-
N-[[4-(methoxycarbonyl)benzyl]sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
comparison of specificity with five additional trypsin-like serine-proteases
N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
N2-(3,5-dimethoxyphenyl)naphthalene-2,6-dicarboxamide
-
-
N2-(3-chlorobiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
N2-(4-(aminomethyl)phenyl)naphthalene-2,6-dicarboxamide trifluoroacetate
-
-
N2-phenylnaphthalene-2,6-dicarboxamide
-
-
naproxen
-
reduces enzyme secretion in chondral and synovial cultures downregulating the PA/plasmin system
NCI004367
-
-
NCI0135766
-
-
NCI0144205
-
-
NCI0666712
-
-
PA inhibitor type 1
-
PAI-1, effects of uPA-PAI-1 are abrogated by the nitric-oxide synthase inhibitor N-D-nitro-L-arginine methyl ester. Dramatically elevated levels in case of acute lung injury
-
PAI-2
-
i.e. plasminogen activator inhibitor type 2, cell-surface enzyme:PAI-2 complex formation is reflective of complete enzyme inhibition, kinetic analysis of inhibition
-
PD 098059
-
hepatocyte growth factor-mediated uPA secretion by Hep-G2 cells is reduced with increasing concentrations of PD 098059
PD98059
-
the ERK MAP kinase inhibitor dramatically reduces the uPA expression in the frozen-thawed porcine uterus endometrial epithelium cells
penicilloic acid
-
-
Pentamidine
-
-
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
-
-
phenethylsulfonamidino-D-seryl-L-alanyl-L-argininal
-
-
phenylmethanesulfonyl fluoride
-
-
plasminogen activator inhibitor
-
PAI-1
-
plasminogen activator inhibitor 1
Plasminogen activator inhibitor 2
-
-
-
plasminogen activator inhibitor type-1
plasminogen activator inhibitor-1
plasminogen activator inhibitor-2
Plumbagin
-
leads to uPA inhibition and downregulation, inhibits adhesion, migration and invasion in HepG2 cells
Protease nexin I
-
-
-
Protein C inhibitor
-
-
-
Soybean trypsin inhibitor
-
-
-
staphylokinase
-
competitively inhibits plasminogen activation by endogenous uPA. The N-terminal residues of staphylokinase are important for inhibition
-
thieno[2,3-b]pyridine-2-carboxamidine
-
APC-7538
trans-3,4'-dimethyl-3-hydroxyflavanone
-
i.e. t-flavanone, a synthetic compound with hair growth enhancing activity that is effective against male pattern alopecia, inhibits the enzyme on the surface of keratinocytes, overview
trans-diphenyl N-(N-benzyloxycarbonyl-D-seryl-L-alanyl)amino-(4-(guanylmethyl)-cyclohexyl)methanephosphonate
-
50% inhibition at 0.0011 mM
tripeptidyl diphenyl phosphonates
-
irreversible inhibition
Trypsin
-
-
-
TX-1877
-
hypoxic cell radiosensitizer. Treatment of nude mice bearing subcutaneously or orthotopically implanted human colon cancer cell lines HCT-116 and HT-29 with TX-1877, irradiation or TX-1877 with irradiation results in significant inhibition of matrix metalloproteinase-9 and uPA. Treatments also inhibit the para-aortic lymph node metastasis, however, do not prolong the survival in orthotopic model. In the subcutaneous model, tumors treated with TX-1877 and irradiation show significant reductions in volume
type-1 plasminogen activator inhibitors
-
primary endogenous inhibitors
-
upain-1
-
competitive, no inhibition of the pro-uPA
WXC-340
-
a selective u-PA inhibitor
-
[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]acetic acid
-
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,3,8-trihydroxy-6-methylanthraquinone
-
i.e. emodin, an active compound of aloe. Emodin increases the fibrinolytic activity of fibroblast cells in a dose-dependent manner, linked to increased uPA activity and uPA gene up-regulation. Emodin also induces up-regulation of uPA inhibitor PAI-1. Up-regulations are independent of emodin's effect on nuclear factor kappaB. The effect on the uPA system may be via generation of reactive oxygen species
Ile-Ile
-
an Ile-Ile or Ile-Val dipeptide can induce limited enzyme activity in the single-chain zymogen form of uPA or its K158A variant, which cannot be activated proteolytically
Ile-Val
-
an Ile-Ile or Ile-Val dipeptide can induce limited enzyme activity in the single-chain zymogen form of uPA or its K158A variant, which cannot be activated proteolytically
integrin alpha v beta3
-
binds specifically to the enzyme and is required for plasminogen activation, overview
-
interleukin beta
-
significantly induces uPA expression and activity via protein kinase Calpha-dependent JNK1/2 and NIK cascades. Induction is inhibited by pretreatment with the inhibitors of JNK1/2, SP600125, of protein kinase C, Ro31-8220 and Go6976, or of nuclear factor kappaB, helenalin, and by transfection with dominant negative mutants of protein kinase C alpha, NIK, and IKKbeta, and siRNAs of JNK1/2 and p65
-
phorbol 12-myristate 13-acetate
-
stimulation of dental pulp cells by tumor necrosis factor-alpha results in increased uPA activity. Tumor necrosis factor-alpha-induced PA release is enhanced in the presence of phorbol 12-myristate 13-acetate
SB 203580
-
pretreatment of Hep-G2 cells with SB 203580 increases hepatocyte growth factor-mediated uPA secretion by 50-60%
tumor necrosis factor-alpha
-
stimulation of dental pulp cells results in increased uPA activity. Tumor necrosis factor-alpha-induced PA release is enhanced in the presence of phorbol 12-myristate 13-acetate
-
UK-356202
-
rapid, sensitive and selective method for detection in human plasma
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.053
Benzyloxycarbonyl-Gly-Gly-Arg-amino-4-trifluoromethylcoumarin
-
-
0.052 - 0.6
GSGRSA
0.03 - 3.8
HYGRSA
0.053 - 0.452
L-pyroGlu-Gly-L-Arg-4-nitroanilide
0.08
L-pyroGlu-Gly-L-Arg-p-NA
-
pH 8.8, 37C
0.297 - 0.608
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
0.014 - 2.2
PFGRSA
0.000243 - 0.017
plasminogen
0.1 - 0.13
pyroGlu-Gly-Arg-4-nitroanilide
0.13 - 2.18
QRGRSA
0.051 - 0.089
S2444
0.13 - 2.3
YGAKAY
additional information
additional information
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0075 - 0.0113
L-pyroglutamyl-glycyl-L-arginine 4-nitroanilide hydrochloride
0.0383 - 14.1
plasminogen
0.73 - 773
pyroGlu-Gly-Arg-4-nitroanilide
0.0077 - 350
S2444
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.12 - 99
pyroGlu-Gly-Arg-4-nitroanilide
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0039
2-(1-hydroxynaphthalen-2-yl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0019
2-(2,6-dihydroxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.00028
2-(2-hydroxy-3-bromo-5-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.00025
2-(2-hydroxy-3-bromophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.00055
2-(2-hydroxy-3-fluorophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0036
2-(2-hydroxy-3-methoxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.008
2-(2-hydroxy-3-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0009
2-(2-hydroxy-3-nitrophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.013
2-(2-hydroxy-4-diethylaminophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0036
2-(2-hydroxy-4-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0037
2-(2-hydroxy-5-bromophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0005
2-(2-hydroxy-5-chlorobiphenyl-3-yl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0028
2-(2-hydroxy-5-fluorophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0036
2-(2-hydroxy-5-methoxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0075
2-(2-hydroxy-5-methylphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0033
2-(2-hydroxy-5-nitrophenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0004
2-(2-hydroxybiphenyl-3-yl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.0055
2-(2-hydroxyphenyl)-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.00018
2-(4-chloro-7-(2-cyano-6-methoxyphenyl)isoquinolin-1-yl)guanidine
-
-
0.0001
2-(4-chloro-7-(2-methoxyphenyl)isoquinolin-1-yl)guanidine
-
-
0.000083
2-(4-chloro-7-(3-methoxyphenyl)isoquinolin-1-yl)guanidine
-
-
0.0001
2-(7-(1,3-benzodioxol-5-yl)-4-chloroisoquinolin-1-yl)guanidine
-
-
0.00034
2-(7-(1,3-benzodioxol-5-yl)isoquinolin-1-yl)guanidine
-
-
0.0004
2-(7-phenylisoquinolin-1-yl)guanidine
-
-
0.055
2-phenyl-1-H-benzoimidazole-5-carboxamidine
-
pH 7.4, 37C
0.00002
2-[2-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
pH 8.8, 25C
0.000084
2-[2-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide
-
pH 8.8, 25C
0.000038
2-[3-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)propyl]isothiourea hydrobromide
-
pH 8.8, 25C
0.00001
2-[3-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy]propyl)isothiourea hydrobromide
-
pH 8.8, 25C
0.0065 - 0.219
3-(1-carbamimidoylpiperidin-3-yl)-L-alanine
0.00248 - 0.045
3-(1-carbamimidoylpiperidin-4-yl)-L-alanine
0.0042
3-(2-bromoethoxy)-7-nitro-1H-isochromen-1-one
-
pH 8.8, 25C
0.014
3-(3-bromopropoxy)-4-trifluoroacetyl-1H-isochromen-1-one
-
pH 8.8, 25C
0.0043
3-(3-bromopropoxy)-7-nitro-1H-isochromen-1-one
-
pH 8.8, 25C
0.000009
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)-5-methoxybenzoic acid
-
-
0.000037
3-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
-
0.000082
4-(4-chloro-1-((diaminomethylene)amino)isoquinolin-7-yl)benzoic acid
-
-
0.0395
4-aminobenzamidine
-
pH 7.4, 37C, mature uPA
0.00021
4-iodobenzo[b]thiophene-2-carboxamidine
-
pH 7.4, 37C
0.000139
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
-
pH 8.8, 37C
0.000631
6-carbamimidoyl-N-phenyl-2-naphthamide
-
pH 8.8, 37C
0.065
7-amino-3-(2-bromoethoxy)-1H-isochromen-1-one
-
pH 8.8, 25C
0.00063
7-methoxy-8-[1-(methylsulfonyl)-1H-pyrazol-4-yl]naphthalene-2-carboximidamide
-
pH 7.4, 37C
0.005
amiloride
-
pH 7.4, 37C, mature uPA
0.097
benzamidine
-
pH 7.4, 37C
0.0023
benzo[b]thiophene-2-carboxamidine
-
pH 7.4, 37C
0.0063
D-Ser-Ala-Arg-NH-(CH2)5-NH2
-
pH 8.8, 37C
0.00041
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
pH 8.8, 37C
0.0004 - 0.0153
mupain-1
0.00004
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
pH 8.8, 37C
0.0000077 - 0.0077
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
0.013
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
-
0.02
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
-
0.036
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
-
0.018
N-[(4-aminobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
-
0.0076
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
0.023
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
-
0.01
N-[(4-methylbenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
0.024
N-[(4-nitrobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
-
0.0014
N-[3-(2-bromoethoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
pH 8.8, 25C
0.000034
N-[3-(3-bromopropoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide
-
pH 8.8, 25C
0.0000006
N-[4-(aminomethyl)phenyl]-6-carbamimidoyl-4-(pyrimidin-2-ylamino)naphthalene-2-carboxamide
-
pH 7.4, 37C
0.018
N-[[4-(methoxycarbonyl)benzyl]sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
0.000002 - 0.000028
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal
0.063
thieno[2,3-b]pyridine-2-carboxamidine
-
pH 7.4, 37C
0.0022
upain-1
-
pH 7.4, 37C, mature uPA
additional information
additional information
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000035
1-[(N-benzylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.013
1-[3'-([3,5-difluoro-6-[5-methyl-2-(1H-tetrazol-1-yl)phenoxy]pyridin-2-yl]oxy)biphenyl-3-yl]methanamine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000098
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
0.0027
2-[(6-[[3',5-bis(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000023
2-[(6-[[3'-(aminomethyl)-5-hydroxybiphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00054
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-3-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00068
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(propan-2-yl)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00022
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methoxybenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00024
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.0013
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-nitrobenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0035
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-5-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.026
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-6-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00084
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000025
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0001
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[[2-(dimethylamino)ethyl](methyl)amino]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.03
2-[(6-[[4'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000089
2-[(6-[[4-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000039
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.000015
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-4-[3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.03
2-[(6-[[6-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.00013
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(methylamino)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0009
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(morpholin-4-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000065
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoro-4-(piperazin-1-yl)pyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00053
2-[[6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-4-(dimethylamino)-3,5-difluoropyridin-2-yl]oxy]-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.02
3-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.03
3-[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]propanoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000072
4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide
0.03
4-(dimethylamino)-2-[[6-([3'-[(dimethylamino)methyl]biphenyl-3-yl]oxy)-3,5-difluoropyridin-2-yl]oxy]benzoic acid
0.0002
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
Homo sapiens
-
pH 8.8, 37C
0.0026
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.013
6-carbamimidoyl-N-phenyl-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.02
6-cyano-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.0021
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.0041
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.004
6-methoxy-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.019
6-methoxy-N-(3'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.0026
6-methoxy-N-(3'-nitrobiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.0069
6-methoxy-N-(3'-nitrobiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.012
6-methoxy-N-(4'-methoxybiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.023
6-methoxy-N-(4'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.0123
amiloride
Homo sapiens
-
pH 7.4, 37C
0.0000089
antibody IgG(DS2)
Homo sapiens
-
pH 7.4, 22C
-
0.0000067
antibody scFv(DS2)
Homo sapiens
-
pH 7.4, 22C
-
0.0000034
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
Homo sapiens
-
pH 8.8, 37C
0.0000067
di-(4-acetamidophenyl) 1-[(N-benzyloxycarbonyl-D-seryl)-Lalanyl]amino-2-[4-(guanidino)phenyl]-ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.000008
diphenyl 1-[(N-2-acetoadamantanyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000069
diphenyl 1-[(N-2-acetothiophenyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000026
diphenyl 1-[(N-benzenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000043
diphenyl 1-[(N-benzoyloxycarbonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.000005
diphenyl 1-[(N-benzoylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000058
diphenyl 1-[(N-naphthalenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.000006
diphenyl 1-[(N-o,o-dimethylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000044
diphenyl 1-[(N-o-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000066
diphenyl 1-[(N-p-bromobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000062
diphenyl 1-[(N-p-cyanobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000058
diphenyl 1-[(N-p-methoxybenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.000007
diphenyl 1-[(N-p-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000015
diphenyl 1-[(N2-thiophenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
Mus musculus
-
pH 8.8, 37C
0.0000031
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
Homo sapiens
-
pH 8.8, 37C
0.016
methyl 4'-(2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.031
methyl 4'-(6-amino-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.011
methyl 4'-(6-bromo-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.0036
methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.007
methyl 4'-(6-chloro-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.009
methyl 4'-(6-cyano-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.004
methyl 4'-(6-methoxy-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.0028
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.016
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-4-carboxylate
0.0098
methyl 4'-(naphthalene-2-sulfonamido)biphenyl-4-carboxylate
Homo sapiens
-
pH 8.8, 37C
0.014
methyl 6-(3'-(methoxycarbonyl)biphenyl-4-ylcarbamoyl)-2-naphthoate
Homo sapiens
-
pH 8.8, 37C
0.008
N-(2,4'-dimethoxybiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.031
N-(3',4'-dimethoxybiphenyl-4-yl)-6-methoxy-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.008
N-(3',4'-dimethoxybiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.062
N-(3'-aminobiphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.0098
N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 8.8, 37C
0.031
N-(3'-methoxybiphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.0012
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
Homo sapiens
-
pH 8.8, 37C
0.031
N-(biphenyl-4-yl)-6-methoxynaphthalene-2-sulfonamide
Homo sapiens
-
pH 8.8, 37C
0.0064
N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 8.8, 37C
0.0024
N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 8.8, 37C
0.0029
N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 8.8, 37C
0.03
N2-(3,5-dimethoxyphenyl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 8.8, 37C
0.0081
N2-(3-chlorobiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 8.8, 37C
0.045
N2-(4-(aminomethyl)phenyl)naphthalene-2,6-dicarboxamide trifluoroacetate
Homo sapiens
-
pH 8.8, 37C
0.015
N2-phenylnaphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 8.8, 37C
0.0113
NCI004367
Homo sapiens
-
pH 7.4, 37C
0.0063
NCI0135766
Homo sapiens
-
pH 7.4, 37C
0.0284
NCI0144205
Homo sapiens
-
pH 7.4, 37C
0.009
NCI0666712
Homo sapiens
-
pH 7.4, 37C
0.0081
[2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]phenyl]acetic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5 - 9.5
-
phosphorylated uPA
7.6
-
assay at
8
-
assay at
8.3
-
assay at
8.5 - 9
-
-
8.8 - 9.5
-
nonphosphorylated uPA
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
25
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
silencing of transmembrane protein Notch1 by siRNA results in significant reduction in the expression of uPA and matrix metalloproteinase-9 gene transcripts. Knock-down of Notch also reduces the mRNA expression and protein levels of uPA and matrix metalloproteinase-9
Manually annotated by BRENDA team
-
melanoma cell
Manually annotated by BRENDA team
-
uPA shows extensive colocalization with alpha-granule proteins in both cultured Quebec platelet disease megakaryocytes and platelets, and with plasminogen in Quebec platelet disease platelets
Manually annotated by BRENDA team
-
plasma cell
Manually annotated by BRENDA team
-
a murine microglial cell line
Manually annotated by BRENDA team
-
standard model of the balloon catheter injury of the carotid. Periadventitial application of recombinant uPA significantly reduces lumen size and vessel area encompassed by the external lamina both 1 and 4 days after treatment.In fallatory cells accumulate in the arterial adventitia at both 1 and 4 days after uPA treatment. Four days after injury in uPA-treated arteries, 3 proinflammatory and 2 oxidation-related genes are differentially expressed
Manually annotated by BRENDA team
-
very low enzyme content
Manually annotated by BRENDA team
-
primary
Manually annotated by BRENDA team
-
pulmonary arterial
Manually annotated by BRENDA team
-
outer root sheath keratinocyte of vibrissa follicle
Manually annotated by BRENDA team
-
uPA, seprase and pipeptidylaminopeptidase IV immunoreactivity is found in dysplastic and cancer cells as well as in stromal cells adjacent to dysplasia and cancer sites, but not in normal epithelium. There is a significant association between uPA expression and sex, tumor size and histological classification in carcinomas. Squamous cell carcinoma lines display higher levels of uPA, seprase and dipeptidylaminopeptidase IV than normal esophageal epithelial cell lines
Manually annotated by BRENDA team
-
human recombinant uPA induces stem cell migration. Retrovirus-mediated overexpression of uPA and uPA receptor in neuroblastoma NB-1691 cells induced robust migration of stem cells toward NB-1691 cell-conditioned media, compared with media derived from wild-type NB-1691 cells. Depletion of uPA from PC-3 prostate cancer cell-conditioned medium blocks stem cell migration
Manually annotated by BRENDA team
-
high enzyme level
Manually annotated by BRENDA team
-
primary
Manually annotated by BRENDA team
-
a hepatic stellate cell line
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
silencing of transmembrane protein Notch1 by siRNA results in significant reduction in the expression of uPA and matrix metalloproteinase-9 gene transcripts. Knock-down of Notch also reduces the mRNA expression and protein levels of uPA and matrix metalloproteinase-9
Manually annotated by BRENDA team
-
human lung cancer cell line H1415, activation of uPA and uPA receptor in malignant solid tumors augments neural and mesenchymal stem cell tropism. Expression levels of uPA receptor on human solid tumor cell linescorrelates with levels of uPA and soluble uPA receptor in tumor cell-conditioned media
Manually annotated by BRENDA team
-
lung fibroblast cell line
Manually annotated by BRENDA team
-
subline of MDA-MB-231, stably transfected with the bacterial lacZ gene
Manually annotated by BRENDA team
-
CD34+ progenitor cells express normal amounts of uPA, while their differentiation into megakaryocytes results in abnormally increased expression of the uPA gene but not the flanking genes for vinculin or calcium/calmodulin-dependent protein kinase IIgamma on chromosome 10. uPA shows extensive colocalization with alpha-granule proteins in both cultured Quebec platelet disease megakaryocytes and platelets, and with plasminogen in Quebec platelet disease platelets
Manually annotated by BRENDA team
-
uPA localizes strongly to natural killer cells of the placental bed, especially at 8-10 weeks of gestation. uPA activity is similar in uterine natural killer cell culture supernatant compared with total unseparated decidual cells. uPA receptor in uterine natural killer cell lysates is significantly stronger than in total decidual cell lysates. Inhibitors PAI-1 and PAI-2 are not detected in uterine natural killer cell culture supernatants
Manually annotated by BRENDA team
-
retrovirus-mediated overexpression of uPA and uPA receptor in neuroblastoma NB-1691 cells induced robust migration of stem cells toward NB-1691 cell-conditioned media, compared with media derived from wild-type NB-1691 cells
Manually annotated by BRENDA team
-
activation of uPA and uPA receptor in malignant solid tumors augments neural and mesenchymal stem cell tropism. Expression levels of uPA receptor on human solid tumor cell lines correlates with levels of uPA and soluble uPA receptor in tumor cell-conditioned media
Manually annotated by BRENDA team
-
activation of uPA and uPA receptor in malignant solid tumors augments neural and mesenchymal stem cell tropism. Expression levels of uPA receptor on human solid tumor cell lines correlates with levels of uPA and soluble uPA receptor in tumor cell-conditioned media
Manually annotated by BRENDA team