3.4.21.106: hepsin
This is an abbreviated version!
For detailed information about hepsin, go to the full flat file.
Word Map on EC 3.4.21.106
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3.4.21.106
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prostate
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matriptase
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medicine
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hai-1
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prostasin
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trypsin-like
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ttsps
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pro-hgf
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amacr
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tmprss3
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uromodulin
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biotechnology
- 3.4.21.106
- prostate
- matriptase
- medicine
- hai-1
- prostasin
-
trypsin-like
-
ttsps
- pro-hgf
- amacr
-
tmprss3
-
uromodulin
- biotechnology
Reaction
cleavage after basic amino-acid residues, with Arg strongly preferred to Lys =
Synonyms
hepsin, S01.224, TMPRSS1, transmembrane serine protease 1, type II transmembrane serine protease
ECTree
3.4.21.106 hepsinAdvanced search results
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results (Inhibitors
Inhibitors on EC 3.4.21.106 - hepsin
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(S)-N-(4-bromobenzyl)-4-(3-(3-carbamimidoylphenyl)-2-(naphthalene-2-sulfonamido)propanoyl)piperazine-1-carboxamide
inhibitor shows potency and selectivity for hepsin over matriptase and hepatocyte growth factor activator
1-[6-(6-methyl-3H-indol-2-yl)pyridin-2-yl]cyclohexan-1-ol
compounds exhibits inhibition of invasion and migration of hepsin-overexpressing cell line. The selective inhibition of hepsin is likely due to interactions of the midine group at the S1 site with the cyclohexyl ring from the 2-aryl group projecting towards the S1' site and the tert-hydroxyl group interacting with His57 side-chain
4-(2-aminoethyl)-benzenesulfonylfluoride hydrochloride
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residual hepsin activity: 0%
9-fluorenylmethyloxycarbonyl-NR-ketobenzothiazole
potent and selective inhibitor for hepsin over matriptase
anthralin
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at 0.067 mM anthralin the hepsin activity is reduced by more than 70%
CaCl2
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43% inhibition at 1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
dithiothreitol
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94% inhibition at 10 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
E64
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31% inhibition at 0.1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
EDTA
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8% inhibition at 1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
hepatocyte growth factor activator inhibitor-1
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potent inhibitor of hepsin activity
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hepatocyte growth factor activator inhibitor-1-derived Kunitz domain inhibitor
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KD1, inhibits cleavage of laminin-332 in a dose-dependent manner
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hepatocyte growth factor activator inhibitor-1B
potent inhibitor of hepsin
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MgCl2
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21% inhibition at 1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
N-alpha-p-tosyl-L-lysine chloromethyl ketone
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12% inhibition at 0.1 mM, with t-butyloxycarbonylc-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
N-ethylmaleimide
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25% inhibition at 1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
N-tosyl-L-phenylalanine chloromethyl ketone
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13% inhibition at 0.1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]-N2-(20-[3,3-dimethyl-5-sulfo-2-[(1E)-3-[(4E)-4-[(2E)-2-(1,3,3-trimethyl-5-sulfo-1,3-dihydro-2H-indol-2-ylidene)ethylidene]cyclohex-1-en-1-yl]prop-1-en-1-yl]-3H-indolium-1-yl]-16-oxo-4,7,10,13-tetraoxa-15-azaicosan-1-oyl)-L-leucinamide
Leu-Arg dipeptide, attached to dye SulfoCy7. Compound shows 1000fold selectivtiy for hepsin over matriptase and selective uptake and retention in hepsin-overexpressing cells
N2-acetyl-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]-L-leucinamide
inhibitor based on tetrapeptide hepsin inhibitor acetyl-KQLR-ketothiazole. Hepsin affinity of the (R)-epimer is similar to that of the corresponding (S)-epimer
N2-acetyl-N-[5-carbamimidamido-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-L-leucinamide
inhibitor based on tetrapeptide hepsin inhibitor acetyl-KQLR-ketothiazole. Hepsin affinity of the (R)-epimer is similar to that of the corresponding (S)-epimer
NaN3
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34% inhibition at 1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
PEGylated Kunitz domain-1
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potent hepsin active site inhibitor derived from hepatocyte growth factor activator inhibitor-1
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serpinB12
forms a covalent complex with hepsin. Hepsin cleaves the reactive-site loop after the Arg residue
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antithrombin III
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76% inhibition at 0.003 mM, 1U/ml heparin enhances inhibition
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hepatocyte growth factor activator inhibitor-2
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potent inhibitor of hepsin activity
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hepatocyte growth factor activator inhibitor-2
potent inhibitor of hepsin
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leupeptin
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96% inhibition at 0.1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
ZnSO4
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59% inhibition at 1 mM, with t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide as substrate
additional information
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no inhibition by soybean trypsin inhibitor and tissue factor pathway inhibitor
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additional information
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hepatocyte growth factor activator inhibitor 1 and hepatocyte growth factor activator inhibitor 2
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additional information
antibody hH35 potently inhibits hepsin enzymatic activity at nanomolar concentrations, showing non-linear, slow, tight-binding inhibition
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additional information
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antibody hH35 potently inhibits hepsin enzymatic activity at nanomolar concentrations, showing non-linear, slow, tight-binding inhibition
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additional information
synthesis of a heterobivalent inhibitor, targeting both hepsin and prostate-specific membrane antigen, EC 3.4.17.21. The compound is based on an amidine-containing indole analog linked with Lys-urea-Glu for binding to prostate-specific membrane antigen, and the optical dye SulfoCy7. Compound shows selective binding and retention in both prostate-specific membrane antigen and hepsin high-expressing cells
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