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1-benzyl-1H-pyrazole-4-carboxylic acid 4-carbamimidoyl-benzylamide
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ASP-440, small molecule inhibitor of plasma kallikrein
2-mercaptoethanol
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inhibition of prekallikrein activation
2-[3'-acetyl-5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2'-fluoro-6-hydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3',6-dihydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-carbamoyl-6-hydroxybiphenyl-3-yl]butanedioic acid
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inhibitor with the best potency and selectivity profile for plasma kallikrein versus related serine proteases. This compound is highly stable in vivo and could be further developed for the treatment and inflammatory or coagulation disorders. Pharmacokinetic data
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-cyano-6-hydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-4'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methoxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methylbiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methoxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methylbiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methoxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methylbiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
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alpha 2 macroglobulin
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alpha1-antiprotease
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alpha1-proteinase inhibitor-Leu-Gly-Arg
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mutant of serpin alpha1-proteinase inhibitor with exchange at P3, P2 and P1 position, fast complexing, inhibition kinetics
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alpha1-proteinase inhibitor-Pro-Phe-Arg
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mutant of serpin alpha1-proteinase inhibitor with exchange at P3, P2 and P1 position, inhibition kinetics
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alpha2-Macroglobulin
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Alzheimer's amyloid beta-protein precursor
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weak inhibition
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antithrombin
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inhibition by antithrombin is 3.4fold improved by heparin, forming a ternary complex with antithrombin
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Bauhinia unglata factor Xa inhibitor
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Bauhinia ungulata factor Xa inhibitor protein
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Bauhinia variegata trypsin inhibitor protein
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BCX4161
low nanomolar inhibitory potency
bicyclic peptide Ac-CiS1F2[Aze]3Y4[HArg]5Cii[Ala(PsiCH2-NH)]6H7Q8D9L10Ciii
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bicyclic peptide Ac-CiS1W2P3A4R5CiiL6H7Q8D9L10Ciii
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bovine dermatan sulfate
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68% inhibition at
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C1 esterase inhibitor
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C1 inhibitor
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increased levels of kallikrein-C1 inhibitor complex are independently associated with increased risk for all-cause mortality and the combined endpoint of all-cause mortality or recurrent troponin T-positive events in patients with admission troponin T greater than/equal 0.05 ng/mL
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cysteine
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inhibition of prekallikrein activation
D-Arg-Hph-Arg-CH2OCH2CF3
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D-Arg-Phe-Arg-CH2OCH2CF3
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D-Arg-Phe-Arg-Ser-NH2
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D-Phe-Phe-Arg-chloromethylketone
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complete inhibition at 0.01 mM
D-Pro-Cha-ArgOH-CH2OCH2CF3
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D-Pro-Phe-Arg-CH2OCH2CF3
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diisopropylfluorophosphate
diphenylcarbamoylfluoride
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dithiothreitol
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inhibition of prekallikrein activation
DX-88
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DX-88 has a strong neuroprotective effect in the early phases of brain ischemia preventing reperfusion injury and indicates that inhibition of plasma kallikrein may be useful tool in the strategy aimed at reducing the detrimental effects linked to reperfusion
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ecotin
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ecotin with mutation H53P in the 50s loop, mutations S82W/T83N/M84R/M85R/A86S in the 80s loop and mutations R108S/N110S in the 100s loop is a high-affinity and highly specific plasma kallikrein inhibitor. Specifically inhibits contact activation of human plasma at the level mediated by plasma kallikrein. Discriminates between enzyme and zymogen. Partial thromboplastin time inhibition can be rescued by addition of PKal
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ecotin-plasma kallikrein
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highly specific inhibitor of active plasma kallikrein
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Elastase
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of human neutrophils, degrades kininogen itself to kinin-containing fragments and therefore quenches the kininogen degeneration/bradykinin generation by plasma kallikrein
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ferritin
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high-molecular weight kininogen is a ferritin-binding protein, binding to the modified light chain of activated kininogen. Binding to kininogen retards the release of bradykinin by inhibition of kallikrein, no inhibition with substrates other than kininogen, binding mechanism, inhibition by holo- and apoferritin
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glutathione
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inhibition of prekallikrein activation
heparin
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improves inhibition by other enzyme inhibitor 1.4-3.4fold, the enzyme binds to a heparin-matrix, but its secondary structure is not modified by heparin, circular dichroism, overview
hepatocyte growth factor activator inhibitor-1
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i.e. HAI-1, Kunitz type inhibitor specific for serine proteases, relatively weak inhibition
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hepatocyte growth factor activator inhibitor-1B
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splicing variant of hepatocyte growth factor activator inhibitor-1, Kunitz type inhibitor specific for serine proteases, relatively weak inhibition
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HgCl2
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inhibition of prekallikrein activation
human C1 esterase inhibitor
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63% inhibition at 0.04 mg/ml
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human IgG1 monoclonal antibody DX-2930
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N-alpha-tosyl-D,L-homophenylalanine-4-anilide hydrochloride
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also known as Pefabloc PK, inhibits plasma kallikrein exclusively
N-[(6-amino-2,4-dimethylpyridin-3-yl)methyl]-1-[[4-(1H-pyrazol-1-ylmethyl)phenyl]methyl]-1H-pyrazole-4-carboxamide
low nanomolar inhibitory potency
o-aminobenzoyl-FESPLRINIIKE-N-(2,4-dinitrophenyl)-ethylene diamine
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competitive inhibitors, based on the Bauhinia bauhinioides inhibitor protein reactive site sequence
o-aminobenzoyl-RPGLPVRFESPL-N-(2,4-dinitrophenyl)-ethylene diamine
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competitive inhibitors, based on the Bauhinia bauhinioides inhibitor protein reactive site sequence
Oxyuranus microlepidotus inhibitor
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p-Carboethoxyphenyl epsilon-guanidine caproate
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plasma kallikrein serine protease inhibitor
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highly specific
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plasma kallikrein-specific Kunitz domain inhibitor
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Protein C inhibitor
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Soybean trypsin inhibitor
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specific serine protease inhibitor protein from Bauhinia bauhinioides seeds
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Swartzia pickellii trypsin inhibitor
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purified from seeds, serine protease inhibitor, contains a glycosylation site at Asn38, Kunitz type, but contains only 1 disulfide bridge
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taicatoxin serine protease inhibitor
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broad spectrum inhibitor with most potent inhibitory activity observed against plasma kallikrein
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trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-Pyrim)-4-carboxyanilide
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trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-Pic)-octylamide
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trans-4-aminomethylcyclohexanecarbonyl-D-phenylalanyl-PSI(CH2-NH)-4-aminophenyl acetic acid
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PKSI-527 pseudo-peptide analogue, 5% inhibition at 1 mM
trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-4-aminophenyl acetic acid
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i.e. PKSI-527, selective inhibitor, both carbonyl groups of the structure are required
trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-PSI(CH2-NH)-4-aminophenyl acetic acid
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PKSI-527 pseudo-peptide analogue, 7% inhibition at 1 mM
trans-4-aminomethylcyclohexanecarbonyl-PSI(CH2-NH)-L-phenylalanyl-4-aminophenyl acetic acid
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PKSI-527 pseudo-peptide analogue, 20% inhibition at 1 mM
triafestin-1
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isolation and analysis of the enzyme inhibitor from salivary glands of instar nymphs of Triatoma infestans, SwissProt ID A7BJ45, recombinant production in insect or Escherichia coli cells, triafestin-1 specifically interacts with factor XII and high molecular weight kininogen in a Zn2+-dependent manner, and inhibit activation of the kallikrein-kinin system by interfering with the association of factor XII and high molecular weight kininogen with biological activating surfaces as well as inhibiting prekallikrein activation, overview
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triafestin-2
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isolation and analysis of enzyme inhibitors from salivary glands of instar nymphs of Triatoma infestans, SwissProt ID A7BJ46, recombinant production in insect or Escherichia coli cells, triafestin-2 specifically interacts with factor XII and high molecular weight kininogen in a Zn2+-dependent manner, and inhibit activation of the kallikrein-kinin system by interfering with the association of factor XII and high molecular weight kininogen with biological activating surfaces as well as inhibiting prekallikrein activation, overview
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tuna dermatan sulfate
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80% inhibition at
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Type IV collagen
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0.02 mg/ml of collagen causes a slight loss of activity even after 5 hours, whereas with 0.1 mg/ml of collagen, there is an initial rapid decrease of activity to about 40%
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Z-Phe-OH
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inhibition of prekallikrein activation
Zn2+
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inhibits the activation of prekallikrein at concentrations above 0.01 mM, regulatory role
antipain
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inhibition of prekallikrein activation
benzamidine
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C1-inhibitor
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activation of plasma kallikrein and generation of bradykinin are responsible for the angioedema attacks observed with C-1 inhibitor deficiency. C1-inhibitor concentration of greater than 0.001 mM is needed to inhibit 3 nM kallikrein
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C1-inhibitor
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inhibition by C1-inhibitor is 1.4fold improved by heparin
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diisopropylfluorophosphate
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diisopropylfluorophosphate
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diisopropylfluorophosphate
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ecallantide
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also called DX-88, C305H442N86O91S8, potent and specific inhibitor of plasma kallikrein
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human IgG1 monoclonal antibody DX-2930
potently and specifically inhibits plasma kallikrein
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human IgG1 monoclonal antibody DX-2930
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potently and specifically inhibits plasma kallikrein
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human IgG1 monoclonal antibody DX-2930
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potently and specifically inhibits plasma kallikrein
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human IgG1 monoclonal antibody DX-2930
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potently and specifically inhibits plasma kallikrein
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leupeptin
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Soybean trypsin inhibitor
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Soybean trypsin inhibitor
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Soybean trypsin inhibitor
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specific serine protease inhibitor protein from Bauhinia bauhinioides seeds
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Kunitz type, purified 20 kDa protein
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specific serine protease inhibitor protein from Bauhinia bauhinioides seeds
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Kunitz type, purified 20 kDa protein, thermolabile inhibition, optimal at pH 8.0 for trypsin, characterization
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additional information
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inhibitory potential of diverse trans-(4-aminomethylcyclohexanecarbonyl)-derivatives, structure-activity relationship study, overview
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additional information
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no inhibition by hirudin, bdellin, and corn trypsin inhibitor
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additional information
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no inhibition by corn trypsin inhibitor
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additional information
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angiotensin II inhibits plasma prekallikrein activation by 11%. 2-Mercaptoethanol, EDTA, benzamidine, 2-aminoethyl benzenesulfonyl fluoride, antipain or leupeptin have little effect on activation, whereas cysteine inhibits activation by approximately 65% at 10 mM. Incubation with 500 mM des-arg9-bradykinin, bradykinin fragment 1-7 or bradykinin fragment 1-5 inhibit plasma prekallikrein activation on A-549 cells by 6%, 20% and 4%, respectively. Plasma prekallikrein activation on A-549 cells is not significantly inhibited by PlummerÂ’s inhibitor, phosphoramidon, captropril, or apstatin
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additional information
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preplasma kallikrein activation on MeT-5A, NCI-H2052, NCI-H28 and primary murine mesothelial cells is strongly inhibited by 10 mM cysteine, 100 mM bradykinin, 100 mg/ml protamine sulfate and 5 mM novobiocin. Moderate inhibition is observed with 2-mercaptoethanol, 2-aminoethyl benzenesulfonyl fluoride, antipain and leupeptin on most cell lines. Angiotensin II, benzamidine and EDTA do not inhibit activation
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