EC Number   |
Inhibitors |
Structure |
|---|
   3.4.21.106 | (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 |
   |
| 3.4.21.106 | 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 |
|
| 3.4.21.106 | 3,4-dichloroisocoumarin |
94% inhibition at 0.1 mM |
|
| 3.4.21.106 | 4-(2-aminoethyl)-benzenesulfonylfluoride hydrochloride |
residual hepsin activity: 0% |
|
| 3.4.21.106 | 4-amidinophenylmethylsulfonyl fluoride |
complete inhibition at 1 mM |
|
| 3.4.21.106 | 4-methylumbelliferyl p-guanidinobenzoate |
irreversible inhibitor |
|
| 3.4.21.106 | 9-fluorenylmethyloxycarbonyl-NR-ketobenzothiazole |
potent and selective inhibitor for hepsin over matriptase |
|
| 3.4.21.106 | alpha1-Aantichymotrypsin |
residual hepsin activity: 88% |
|
| 3.4.21.106 | alpha1-antitrypsin |
residual hepsin activity: 67% |
|
| 3.4.21.106 | alpha2-antiplasmin |
residual hepsin activity: 1% |
|
