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3.4.21.20: cathepsin G

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

Word Map on EC 3.4.21.20

Reaction

specificity similar to chymotrypsin C =

Synonyms

alpha-protease, cat G, Cat-G, Cat.G, CatG, Cath G, cathepsin G, chymotrypsin-like proteinase, CTSG, More, neutral proteinase, serine protease cathepsin G, Vimentin-specific protease, VSP

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.20 cathepsin G

Inhibitors

Inhibitors on EC 3.4.21.20 - cathepsin G

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
11-oxo-beta-boswellic acid
0.01 mM, 30% cathepsin G activity compared to control
2-(N-methyl)benzylamino-3,1-benzoxazin-4-one
-
strongest inhibition
2-amino-3,1-benzoxazin-4-ones
-
non-covalent complex formation, hydrophobic and basic residues at position 2, kinetics of acylation and desacylation, binding at the enzyme's active site
3-O-acetyl-11-oxo-beta-boswellic acid
0.01 mM, 15% cathepsin G activity compared to control
3-O-acetyl-beta-boswellic acid
0.01 mM, 5% cathepsin G activity compared to control
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
-
-
6-((1'R)-camphanyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
-
6-((1'R,2'S,5'R)-menthyloxycarbonyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
-
6-((1'S)-camphanyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
selective inhibition
6-((1'S,2'R,5'S)-menthyloxycarbonyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
-
6-(benzoyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
selective inhibition
6-(N-tosyl-L-phenylalanyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
-
6-(N-tosyl-L-valinyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
-
-
alpha-1 proteinase inhibitor
-
-
-
alpha-1-antichymotrypsin
-
-
-
alpha1-Aantichymotrypsin
-
alpha1-CT
-
-
alpha1-protease inhibitor
-
-
Alpha1-proteinase inhibitor
-
alpha1alpha2-macroglobulin
-
-
-
alpha2-Macroglobulin
-
aspartyl protease inhibitor pepstatin
-
-
-
benzyloxycarbonyl-Gly-Leu-Phe-chloromethyl ketone
beta-boswellic acid
0.01 mM, 30% cathepsin G activity compared to control
bis(4-ethylphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
-
bis(4-methoxyphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
more potent inhibitor for related proteases than cathepsin G
bis(4-methylphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
-
bis(4-tert-butylphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
-
bis-naphthyl beta-ketophosphoric acid
-
moderately potent, competitive, reversible, the R-isomer occupies the active site of the enzyme
bis[4-(1,1,3,3-tetramethylbutyl)phenyl] [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
3% inhibition, 115 microM
bis[4-(1-methylethyl)phenyl] [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] ([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][(O-tert-butyl-L-threonyl)amino]methyl)phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] [[4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl]([O-tert-butyl-N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-threonyl]amino)methyl]phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
more potent inhibitor for related proteases than cathepsin G
CatG-specific inhibitor I
-
reversible inhibitor
-
cathepsin G inhibitor I
-
chelonianin
-
-
chymostatin
-
-
chymotrypsin inhibitor 1
-
Apis mellifera
-
chymotrypsin inhibitor 2
-
Apis mellifera
-
chymotrypsin inhibitor 3
-
Apis mellifera
-
cysteine protease inhibitor E64
-
-
dermatan sulfate
-
25 kDa, protection of laminin and fibronectin against degradation by cathepsin G
dichloroisocoumarin
-
-
diethyl 1-naphthylmethylphosphonate
-
-
diisopropylfluorophosphate
dinaphthalen-2-yl [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
-
diphenyl (1-[[(benzyloxy)carbonyl]amino]-3-carbamimidamidopropyl)phosphonate
-
-
diphenyl (4-amino-1-[[(benzyloxy)carbonyl]amino]butyl)phosphonate
-
5% inhibition, 221 microM
diphenyl [(4-aminophenyl)[[(benzyloxy)carbonyl]amino]methyl]phosphonate
-
-
diphenyl [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
-
more potent inhibitor for related proteases than cathepsin G
diphenyl [[[(benzyloxy)carbonyl]amino](4-carbamimidoylphenyl)methyl]phosphonate
-
30% inhibition, 112 microM
diphenyl [[[(benzyloxy)carbonyl]amino](6-carbamimidoylnaphthalen-2-yl)methyl]phosphonate
-
5% inhibition, 112 microM
diphenyl [[[(benzyloxy)carbonyl]amino](phenyl)methyl]phosphonate
-
more potent inhibitor for related proteases than cathepsin G
ecotin
-
-
-
Eglin c
furoylsaccharin
-
-
glut-11-oxo-beta-boswellic acid
0.01 mM 20% cathepsin G activity compared to control
heparan sulfate
-
60 kDa, protection of laminin and fibronectin against degradation by cathepsin G
heparin
-
12 kDa, 1:1 binding stoichiometry with cathepsin G, protection of laminin and fibronectin against degradation by cathepsin G
heparin N
-
-
-
heparin S0
-
-
-
heparin S1
-
-
-
heparin S2
-
-
-
heparin S3
-
-
-
high molecular mass kininogen
-
i.e. HK, human, competitive, inhibits platelet activation by the enzyme completely by complex formation with the enzyme
-
JNJ-10311795
inhibitor of cathepsin G and chymase. The possibility to inhibit both cathepsin G and chymase with a single molecule suggests an opportunity in the treatment of asthma and chronic obstructive pulmonary disease
L-1-tosylamido-2-phenylethyl chloromethyl ketone
-
weak inhibition
L-valyl-N-([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][bis[4-(methylsulfanyl)phenoxy]phosphoryl]methyl)-O-tert-butyl-L-threoninamide
-
-
L-valyl-N-[[bis[4-(methylsulfanyl)phenoxy]phosphoryl](4-carbamimidamidophenyl)methyl]-L-threoninamide
-
-
leupeptin
-
-
Lys16-aprotinin
-
monocyte neutrophil elastase inhibitor
-
-
mutant R346F of plasminogen activator inhibitor-1
-
-
-
N-acetyl-L-phenylalanyl-L-valyl-N-([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][bis[4-(methylsulfanyl)phenoxy]phosphoryl]methyl)-O-tert-butyl-L-threoninamide
-
-
N-acetyl-L-phenylalanyl-L-valyl-N-[[bis[4-(methylsulfanyl)phenoxy]phosphoryl](4-carbamimidamidophenyl)methyl]-L-threoninamide
-
-
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe-chloromethylketone
irreversible inhibitor
N-succinyl-L-Val-L-Pro-L-Phe(OPh)2
-
irreversible CatG inhibitor, complete inhibition at 0.01 mM
N-succinyl-L-Val-L-Pro-L-Phe-(OPh)2
irreversible inhibitor
N-tosyl-L-phenylalanine chloromethyl ketone
N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-valyl-N-([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][bis[4-(methylsulfanyl)phenoxy]phosphoryl]methyl)-O-tert-butyl-L-threoninamide
-
-
N-[[bis[4-(methylsulfanyl)phenoxy]phosphoryl](4-carbamimidamidophenyl)methyl]-L-threoninamide
-
two times more active against cathepsin G than against trypsin
Na-tosyl-Phe-chloromethylketone
pepstatin
-
15% inhibition after 30 min at 0.1 mM at 25°C
pepstatin A-penetratin
-
-
-
phenylmethylsulfonyl fluoride
plasma serine protease inhibitor ACT
-
-
-
protease inhibitor PI6
-
-
RG1150
-
i.e. carboxymethyl-benzylamide-dextran derivative, protection of laminin and fibronectin against degradation by cathepsin G
-
RG1192
-
i.e. carboxymethyl-benzylamide-dextran sulfate derivative, protection of laminin and fibronectin against degradation by cathepsin G
-
RG1503
-
i.e. carboxymethyl-dextran sulfate derivative, protection of laminin and fibronectin against degradation by cathepsin G
-
secretory leukocyteprotease inhibitor
-
-
Soybean trypsin inhibitor
-
specific Cat-G inhibitor
-
1 microM, decrease of enzyme activity by 43%
-
squamous cell carcinoma antigen 2
-
-
thrombospondin 1
-
-
-
tosylphenylalanyl chloromethane
-
-
ursolic acid
0.01 mM, 80% cathepsin G activity compared to control
[2-(3-methylcarbamoyl-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
-
-
[2-(3-[(3-benzoylamino-propyl)-methyl-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
-
-
[2-(3-[(piperidin-4-yl)-methyl-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
-
reversible, selective, competitive inhibition
[2-(3-[methyl-(diphenyl-ethylcarbamoyl-methyl)-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
-
strong inhibition
[2-(3-[methyl-(phenethylcarbamoyl-methyl)-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
-
-
[2-(3-[methyl[1-(2-naphthoyl)piperidin-4-yl]amino]carbonyl]-2-naphthyl)-1-(1-naphthyl)-2-oxoethyl]phosphonic acid
0.0005 mM, 10% cathepsin G activity compared to control
[2-[3-(benzyl-methyl-carbamoyl)-naphthalen-2-yl]-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
-
-
[Nphe,Npip,Nleu]SFTI-1
-
0.1 mM
[Phe(4-guanidine)]SFTI-1
-
0.1 mM
additional information
-