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3.4.21.118: kallikrein 8

This is an abbreviated version!
For detailed information about kallikrein 8, go to the full flat file.

Word Map on EC 3.4.21.118

Reaction

cleavage of amide substrates following the basic amino acids Arg or Lys at the P1 position, with a preference for Arg over Lys =

Synonyms

Alzheimers associated protease, brain serine protease 1, GK-8, hK8, kallikrein 8, kallikrein 8 protease, kallikrein-8, kallikrein-related peptidase, kallikrein-related peptidase 8, kallikrein-related peptidase-8, KLK8, KRP/hK8, mK8, neuropsin, NP, ovasin, P1 kallikrein, PRSS19, RGK-8, S01.244, TADG-14, TADG14, tissue kallikrein, type I neuropsin, type II neuropsin

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.118 kallikrein 8

Inhibitors

Inhibitors on EC 3.4.21.118 - kallikrein 8

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4-amidinohenyl)methanesulfonyl 1-fluoride
61% inhibition at 1 mM
1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
compound is a promising lead for development of novel kallikrein-8 inhibitors. It binds stably to the kallikrein-8 S1 binding site
1-(3,5-difluorophenyl)-5-hydroxy-7-(4-hydroxy-3,5-dimethoxyphenyl)-6,7-dihydro-1H-pyrrolo[3,2-b] pyridine-3-carboxylic acid
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i.e. ZINC61720639
2-[[5-(2-chlorophenyl)-4-imino-3-methyl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]sulfanyl]-N-(2,5-dimethoxyphenyl)acetamide
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4,4'-[pentane-1,5-diylbis(oxy)]bis(3,5-dibromobenzenecarboximidamide)
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4-amino-N3-[(2R)-1-(tert-butylamino)-1-oxopropan-2-yl]-N3-(3-chloro-4-fluorophenyl)-2H-pyrrole-3,5-dicarboxamide
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alpha2-antiplasmin
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-
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antipain
Aprotinin
benzamidine
chymostatin
diisopropyl fluorophosphate
2 mM, 100% inhibition
diisopropylfluorophosphate
16% inhibition at 0.1 mM
human alpha1-antichymotrypsin
weak, 16% inhibition at 2 mM
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human alpha1-antitrypsin
weak, 20% inhibition at 10 mM
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leupeptin
murinoglobulin I
24% inhibition at enzyme-inhibitor ratio of 1:2; formation of a SDS-stable complex; i.e. MUG I
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N-(7-amino-1-chloro-2-oxoheptan-3-yl)-4-methylbenzenesulfonamide
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N-[[5-([2-[(4-bromo-2-fluorophenyl)amino]-2-oxoethyl]sulfanyl)-4-methyl-4H-1,2,4-triazol-3-yl]methyl]furan-2-carboxamide
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Ni2+
50% inhibition at 0.011 mM
NP STOP
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neuropsin-specific inhibitor. Single stimulus in S1 during application of NP STOP completely eliminates the late associativity between S0 and S1 synapses. When a strong (four) stimulus in S0 is followed by the application of NP STOP, the late associativity between S0 and S1 synapses is not eliminated
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pefabloc
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phenylmethylsulfonyl fluoride
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Protein C inhibitor
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serine protease inhibitor-3
formation of a SDS-stable complex, bimolecular kinetics; from pyramidal neurons; slowly and tightly binding inhibitor
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serpinB6
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shRNA
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inhibition of endogenous KLK8 expression, reduces cancer cell invasiveness
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trans-epoxysuccinyl-L-leucylamido(4-guanidinobutane)
i.e. E-64, 15% inhibition at 0.1 mM
additional information
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