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(1E,4E)-1-chloro-4-ethenyl-2-(trichloro-lambda4-tellanyl)hepta-1,4,6-trien-3-ol
-
(1R,2S)-2-([(8-hydroxy-5-nitroquinolin-7-yl)methyl]amino)cyclohexane-1-carboxylic acid
-
-
(1S,3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 2,3,6-trideoxy-3-[([[4-([N-[6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl]-L-phenylalanyl-L-lysyl]amino)benzyl]oxy]carbonyl)amino]-a-L-lyxo-hexopyranoside
-
a Phe-Lys-para-aminobenzyloxycarbonyl-doxorubicin prodrug-albumin
(2(1H)-pyridinethionato-kappaS2)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
-
-
(2E)-3-chloro-1-phenyl-2-(trichloro-lambda4-tellanyl)prop-2-en-1-ol
-
-
(2R,3R)-3-(((1S)-1-[(4-carbamimidamidobutyl)carbamoyl]-3-methylbutyl)carbamoyl)oxirane-2-carboxylic acid
-
(2R,3R)-3-(((1S)-3-methyl-1-[(3-methylbutoxy)carbonyl]butyl)carbamoyl)aziridine-2-carboxylic acid
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(2S,3S)-3-(((1S)-1-[(4-([(benzyloxy)carbonyl]amino)butyl)carbamoyl]-3-methylbutyl)carbamoyl)oxirane-2-carboxylic acid
-
(2S,3S)-3-(((1S)-1-[(4-aminobutyl)carbamoyl]-3-methylbutyl)carbamoyl)oxirane-2-carboxylic acid
-
(2S,3S)-3-(((1S)-1-[(4-carbamimidamidobutyl)carbamoyl]-3-methylbutyl)carbamoyl)oxirane-2-carboxylic acid
-
(2S,3S)-3-(((1S)-1-[(7-aminoheptyl)carbamoyl]-3-methylbutyl)carbamoyl)oxirane-2-carboxylic acid
-
(2S,3S)-3-(((1S)-3-methyl-1-[(3-methylbutoxy)carbonyl]butyl)carbamoyl)aziridine-2-carboxylic acid
-
(2S,3S)-3-(((1S)-3-methyl-1-[(3-methylbutyl)carbamoyl]butyl)carbamoyl)oxirane-2-carboxylic acid
-
(2S,3S)-3-([(1S)-1-(benzylcarbamoyl)-3-methylbutyl]carbamoyl)oxirane-2-carboxylic acid
-
(2Z)-1,3-bis(2-methoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
(2Z)-1,3-bis(4-ethoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
-
(2Z)-1,3-bis(4-methoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
-
(2Z)-1,3-diphenyl-4-(trichloro-llambda4-tellanyl)but-2-en-1-one
-
-
(3E)-2-bromo-3-(bromomethylidene)-2-(4-methoxyphenyl)-1-oxa-2l4-telluraspiro[3.5]nonane
-
-
(3E)-2-bromo-3-(bromomethylidene)-2-(4-methoxyphenyl)-1-oxa-2lambda4-telluraspiro[3.5]nonane
-
(3E)-2-chloro-3-(chloromethylidene)-2-(4-methoxyphenyl)-1-oxa-2l4-telluraspiro[3.5]nonane
-
-
(3E)-2-chloro-3-(chloromethylidene)-2-(4-methoxyphenyl)-1-oxa-2lambda4-telluraspiro[3.5]nonane
irreversible inhibition
(3E)-2-chloro-3-(chloromethylidene)-2-(4-methoxyphenyl)-1-oxa-2lambda4-telluraspiro[3.6]decane
-
(3E)-4-chloro-3-([(2Z)-4-methoxy-1-methylidenepenta-2,4-dien-1-yl](dimethyl)-lambda4-tellanyl)-2-methylbut-3-en-2-ol
-
(3E)-4-chloro-3-[dichloro(4-methoxyphenyl)-l4-tellanyl]-2-methylbut-3-en-2-ol
-
-
(5S)-5-([N-[(benzyloxy)carbonyl]-L-phenylalanyl]amino)-7-[(2,6-dimethylbenzoyl)oxy]-6-oxoheptan-1-aminium trifluoroacetate
-
(5S)-5-([N-[(benzyloxy)carbonyl]-L-phenylalany]amino)-6-oxo-7-[(2,4,6-trimethylbenzoyl)oxy]heptan-1-aminium trifluoroacetate
-
(acetatato-kO)[2-(1-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl-kN4)phenyl-kC1](pyridine)palladium(1+)
-
-
(acetatato-kO)[2-(1-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl-kN4)phenyl-kC1](triphenylphosphane)palladium(1+)
-
-
(acetato)(isopropylamine)(2-((2dimethylamino)-methyl)phenyl)Pd(II)
-
-
(benzyl[(8-hydroxy-5-nitroquinolin-7-yl)methyl]amino)acetonitrile
-
-
(chloro)(isopropylamine)(2-((2dimethylamino)methyl)phenyl)Pd(II)
-
-
(chloro)(pryidinyl)(2-((2dimethylamino)methyl)phenyl)Pd(II)
-
-
(chloro)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN1] oxorhenium(V)
-
-
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
-
-
(p-methoxyphenylthiolato-S)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
-
-
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
-
-
(S)-18-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(4-iodo-1H-1,2,3-triazol-1-yl)-12,19-dioxo-3,6,9-trioxa-13-azaicosan-20-yl 2,4,6-trimethylbenzoate
-
(S)-20-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(3-iodophenyl)-1,14,21-trioxo-5,8,11-trioxa-2,15-diazadocosan-22-yl 2,4,6-trimethylbenzoate
-
(S)-20-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-1-(4-iodophenyl)-1,14,21-trioxo-5,8,11-trioxa-2,15-diazadocosan-22-yl 2,4,6-trimethylbenzoate
-
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-(3-iodobenzamido)-2-oxoheptyl 2,4,6-trimethylbenzoate
pH 6, 37°C, ki/Ki (sec-1M-1): 630
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[3-(3-iodophenyl)ureido]-2-oxoheptyl 2,4,6-trimethylbenzoate
pH 6, 37°C, ki/Ki (sec-1M-1): 0.013
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[3-(4-iodophenyl)ureido]-2-oxoheptyl 2,4,6-trimethylbenzoate
pH 6, 37°C, ki/Ki (sec-1M-1): 0.0035
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(3-iodobenzamido)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate
pH 6, 37°C, ki/Ki (sec-1M-1): 280
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(4-iodo-1H-1,2,3-triazol-1-yl)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate
-
(S)-3-[(S)-2-([(benzyloxy)carbonyl]amino)-3-phenylpropanamido]-7-[6-(4-iodobenzamido)hexanamido]-2-oxoheptyl 2,4,6-trimethylbenzoate
pH 6, 37°C, ki/Ki (sec-1M-1): 310
(S)-3-[(S)-2-[(benzyloxycarbonyl)amino]-3-phenylpropanamido]-7-(6-[3-(3-iodophenyl)ureido]hexanamido)-2-oxoheptyl 2,4,6-trimethylbenzoate
-
(S)-3-[(S)-2-[(benzyloxycarbonyl)amino]-3-phenylpropanamido]-7-(6-[3-(4-iodophenyl)ureido]hexanamido)-2-oxoheptyl 2,4,6-trimethylbenzoate
-
(triethylphosphine)gold(I) chloride
-
-
([(8-hydroxy-5-nitroquinolin-7-yl)methyl](methyl)amino)acetonitrile
-
-
([(8-hydroxy-5-nitroquinolin-7-yl)methyl]amino)acetonitrile
-
best performing inhibitor is effective in cell-based in vitro models of tumor invasion, where it significantly abrogates invasion of MCF-10A neoT cells
1,1'-[[3-(5-nitroquinolin-8-yl)furan-2,5-diyl]dibenzene-4,1-diyl]diethanone
-
1,1,3-trichloro-2,4,5,6-tetrahydro-1H-1-benzotellurophene
-
-
1,3,5-triphenyl pyrazole
-
1,3,5-triphenyl-2-pyrazoline
-
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-nitronaphthalen-1-yl)pyrrolidine
-
-
1-(dichloro[(1E)-1-chloro-3-methoxyprop-1-en-2-yl]-l4-tellanyl)-4-methoxybenzene
-
-
1-(dichloro[(1Z,3E,5Z)-2-chloroocta-1,3,5,7-tetraen-1-yl]-lambda4-tellanyl)-4-methoxybenzene
-
1-(dichloro[(Z)-2-chloro-2-phenylethenyl]-l4-tellanyl)-4-methoxybenzene
-
bis-vinylic organotellurane, can be a candidate as a starting compound to design more efficient and specific inhibitors for cathepsin B
1-tosylamide-2-phenylethyl chloromethylketone
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
-
-
1-[4-[3-(5-nitroquinolin-8-yl)furan-2-yl]phenyl]ethan-1-one
-
1-[N-(tert-butoxycarbonyl)-L-phenylalanyl]-3-(ethoxycarbonyl)aziridine-2-carboxylic acid
-
1-[N-(tert-butoxycarbonyl)-L-phenylalanyl]aziridine-2,3-dicarboxylic acid
-
2,12-diethyl-11-methylhexadecyl 2-ethyl-11-methylhexadecyl phthalate
-
isolated from seahorse, Hippocampus Kuda Bleeker, NMR structure determination and analysis, overview
2-(3-chloro-4-fluorophenyl)-1,2-thiazol-3(2H)-one
-
-
2-bromo-4-nitronaphthalen-1-amine
-
-
2-chlorobenzohydrazide
competitive inhibition
2-ethyldecyl 2-ethylundecyl phthalate
-
isolated from seahorse, Hippocampus Kuda Bleeker, NMR structure determination and analysis, overview
2-methoxybenzohydrazide
competitive inhibition
2-methyl-5-nitroquinolin-8-ol
-
2-pentyl-1,2-thiazol-3(2H)-one
-
-
2-phenylisothiazol-3(2H)-one
-
-
2-[(6-([3'-(aminomethyl)biphenyl-3-yl]oxy)-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
-
2A2 monoclonal antibody
-
binds to the epitope EPGYSP sequence, i.e. in the nonapeptide CIAEPGYSP, that is located between amino acid residues 133-138 of cathepsin B in the proximity of the occluding loop, surface plasmon resonance analysis, overview. Binding of 2A2 monoclonal antibody to the cathepsin B/cystatin C complex causes the dissociation of cystatin C from the complex, and binding of the antibody induces a conformational change in cathepsin B, stabilizing its exopeptidase conformation and thus disabling its harmful action associated with its endopeptidase activity
-
3,5-diphenyl-2-pyrazoline
-
3,5-diphenyl-4-amino-1,2,4-triazole
non-competitive inhibition
3-(([(3S)-3-((N-[(4-chloro-2-fluorophenyl)carbonyl]-3-methyl-L-phenylalanyl)amino)-3-cyanopropyl]oxy)methyl)benzoic acid
IC50: 0.000002 mM
3-(([(3S)-3-cyano-3-([3-methyl-N-(phenylcarbonyl)-L-phenylalanyl]amino)propyl]oxy)methyl)benzoic acid
IC50: 0.0000094 mM
3-(([(3S)-3-cyano-3-([N-(diphenylacetyl)-3-methyl-L-phenylalanyl]amino)propyl]oxy)methyl)benzoic acid
IC50: 0.0000018 mM
3-(2-hydroxy-3-methylphenyl)-5-(2-hydroxy-3-methylphenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-(2-methylphenyl)-5-(2-methylphenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-(3-aminophenyl)-5-(3-aminophenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-(3-methylphenyl)-5-(3-methylphenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-(4-chlorophenyl)-5-(4-chlorophenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-(4-methylphenyl)-5-(4-methylphenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-(N-benzyloxycarbonylphenylalanylamido)-DL-1-fluoro-2-butanone
irreversible covalent inhibitor
3-([(2R)-2-cyano-2-([3-methyl-N-(2-methyl-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl)-L-phenylalanyl]amino)ethoxy]methyl)benzoic acid
IC50: 0.0000049 mM
3-([(2R)-2-cyano-2-([3-methyl-N-(3-oxo-2,3-dihydro-1H-inden-5-yl)-L-phenylalanyl]amino)ethoxy]methyl)benzoic acid
IC50: 0.0000053 mM
3-([(2R)-2-cyano-2-([N-(1,1-dimethyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methyl-L-phenylalanyl]amino)ethoxy]methyl)benzoic acid
IC50: 0.0000053 mM
3-methylbutyl N-[(3-methoxy-1,2,4-thiadiazolidin-5-yl)carbamoyl]-L-leucyl-L-prolinate
IC50: 0.367 mM
3-phenyl-5-(3-nitrophenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-phenyl-5-(4-nitrophenyl)-4-amino-1,2,4-triazole
non-competitive inhibition
3-[(5S)-5-cyano-5-([N-(diphenylacetyl)-3-methyl-L-phenylalanyl]amino)pentyl]benzoic acid
IC50: 0.000018 mM
4'''-methylamentoflavone
IC50: 0.00168 mM
4-(([(3S)-3-cyano-3-([N-(diphenylacetyl)-3-methyl-L-phenylalanyl]amino)propyl]oxy)methyl)benzoic acid
IC50: 0.000005 mM
4-(4-nitronaphthalen-1-yl)morpholine
-
-
4-bromochalcone phenyl hydrazone
-
4-chlorochalcone phenyl hydrazone
-
4-hydroxy-2-nonenal
-
0.015 mM, 76% loss of activity, formation of Michael adducts with C29 of A chain and H150 of B chain
4-hydroxybenzohydrazide
competitive inhibition
4-methoxy-3-(3-methoxypropoxy)-1-(5-nitroquinolin-8-yl)pyridin-1-ium
-
4-methoxybenzohydrazide
competitive inhibition
4-methoxychalcone phenyl hydrazone
-
4-methylchalcone phenyl hydrazone
-
4-nitro-L-phenylalanine
inactivation rate is 3.0 mM/min
4-nitrochalcone phenyl hydrazone
-
4-nitronaphthalen-1-amine
-
-
4-nitronaphthalen-1-ol
-
-
5,5'-dithiobis-2-nitrobenzoic acid
-
-
5,7-dihydroxy-2-(4-hydroxy-3-[7-hydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-8-yl]phenyl)-4H-chromen-4-one
IC50: 0.00175 mM
5,7-dihydroxy-2-(4-hydroxy-3-[7-hydroxy-2-(4-methoxyphenyl)-4-oxo-4H-chromen-8-yl]phenyl)-4H-chromen-4-one
IC50: 0.00168 mM
5,7-dihydroxy-2-(4-hydroxy-3-[7-methoxy-2-(4-methoxyphenyl)-4-oxo-4H-chromen-8-yl]phenyl)-4H-chromen-4-one
IC50: 0.00055 mM
5,7-dinitroquinolin-8-ol
-
-
5-(((2R)-2-cyano-2-[(3-methyl-N-phenyl-L-phenylalanyl)amino]ethoxy)methyl)-2-fluorobenzoic acid
IC50: 0.0000122 mM
5-(4-bromophenyl)-1,3-diphenyl pyrazole
-
5-(4-bromophenyl)-1,3-diphenyl-2-pyrazoline
-
5-(4-bromophenyl)-3-phenyl-2-pyrazoline
-
5-(4-chlorophenyl)-1,3-diphenyl pyrazole
-
5-(4-chlorophenyl)-1,3-diphenyl-2-pyrazoline
-
5-(4-chlorophenyl)-3-phenyl-2-pyrazoline
-
5-(4-methoxyphenyl)-1,3-diphenyl pyrazole
-
5-(4-methoxyphenyl)-1,3-diphenyl-2-pyrazoline
-
5-(4-methoxyphenyl)-3-phenyl-2-pyrazoline
-
5-(4-methylphenyl)-1,3-diphenyl pyrazole
-
5-(4-methylphenyl)-1,3-diphenyl-2-pyrazoline
-
5-(4-methylphenyl)-3-phenyl-2-pyrazoline
-
5-(4-nitrophenyl)-1,3-diphenyl pyrazole
-
5-(4-nitrophenyl)-1,3-diphenyl-2-pyrazoline
-
5-(4-nitrophenyl)-3-phenyl-2-pyrazoline
-
5-([(2R)-2-cyano-2-([3-methyl-N-(3-oxo-1,3-dihydro-2-benzofuran-5-yl)-L-phenylalanyl]amino)ethoxy]methyl)-2-fluorobenzoic acid
IC50: 0.0000041 mM
5-amino-1-(phenylsulfonyl)-1H-pyrazol-3-yl thiophene-2-carboxylate
-
-
5-amino-1-[(4-fluorophenyl)sulfonyl]-1H-pyrazol-3-yl furan-2-carboxylate
-
-
5-amino-1-[(4-fluorophenyl)sulfonyl]-1H-pyrazol-3-yl thiophene-2-carboxylate
-
-
5-amino-1-[(4-methoxyphenyl)sulfonyl]-1H-pyrazol-3-yl thiophene-2-carboxylate
-
-
5-amino-1-[(4-methylphenyl)sulfonyl]-1H-pyrazol-3-yl furan-2-carboxylate
-
-
5-amino-1-[(4-methylphenyl)sulfonyl]-1H-pyrazol-3-yl thiophene-2-carboxylate
-
-
5-chloro-2-(2-chloro-4,5-dimethoxyphenethyl)isothiazol-3(2H)-one
-
-
5-chloro-2-(3-chloro-4-fluorophenyl)-1,2-thiazol-3(2H)-one
-
-
5-chloro-2-pentyl-1,2-thiazol-3(2H)-one
-
-
5-chloro-2-phenylisothiazol-3(2H)-one
-
-
5-nitro-7-((4-[(pyridin-3-yl)methyl]piperazin-1-yl)methyl)quinolin-8-ol
-
-
5-nitro-7-((4-[(pyridin-4-yl)methyl]piperazin-1-yl)methyl)quinolin-8-ol
-
-
5-nitro-N-[(pyridin-2-yl)methyl]quinolin-8-amine
-
-
7'',4'''-dimethylamentoflavone
IC50: 0.00055 mM
7-([(2R)-2-methylpiperidin-1-yl]methyl)-5-nitroquinolin-8-ol
-
-
7-epiclusianone
-
a prenylated benzophenone isolated from pericarp hexane extract of dried fruits of Rheedia brasiliensis
7-[(benzylamino)methyl]-5-nitroquinolin-8-ol
-
-
7-[(ethylamino)methyl]-5-nitroquinolin-8-ol
-
-
8-(4-methylpiperidin-1-yl)-5-nitroquinoline
-
-
8-(morpholin-4-yl)-5-nitroquinoline
-
-
8-hydroxy-5-nitroquinoline-2-carbonitrile
-
8-hydroxy-5-nitroquinoline-7-carboxylic acid
-
-
aceto[2,6-bis[(butylthio-kappaS)methyl]phenyl-kappaC]-,(SP-4-3)Pd(II)
-
-
aceto[2,6-bis[(methylthio-kappaS)methyl]phenyl-kappaC]-,(SP-4-3)Pd(II)
-
-
aceto[2,6-bis[(phenylthio-kappaS)methyl]phenyl-kappaC]-, (SP-4-3)Pd(II)
-
-
acetyl-Asp-Glu-Val-Asp-CHO
-
complete DEVDase activity inhibition in brain cell supernatant
acetyl-Leu-Ile-arginal
IC50: 0.00015 mM
acetyl-Leu-Leu-lysinal
IC50: 0.00013 mM
acetyl-Leu-Phe-arginal
IC50: 0.0011 mM
acetyl-Leu-Phe-lysinal
IC50: 0.0001 mM
acetyl-Leu-Val-lysinal
IC50: 0.000004 mM
acetyl-Phe-Val-arginal
IC50: 0.000039 mM
acetyl-YVAD-chloromethyl ketone
AEBSF
0.2 mM, partial inhibition; 0.2 mM, partial inhibition; 0.2 mM, partial inhibition; 0.2 mM, partial inhibition
AM4299A
irreversible inhibition, IC50: 0.000073 mM
AM4299B
irreversible inhibition, IC50: 0.000130 mM
amentoflavone
IC50: 0.00175 mM
ammonium 1-tribromo-1,3,2-dioxatellurolane
-
-
ammonium 1-trichloro-1,3,2-dioxatellurolane
-
-
ankyrin repeat protein
i.e. DARPin 8h6
-
APC-3316
-
kinetics, pH-dependence of inhibition
APC-5840
-
kinetics, pH-dependence of inhibition
APC-8754
-
kinetics, pH-dependence of inhibition
arsenite
-
i.e. arsenic trioxide, inhibits CatB in glioblastoma cells, 20% inhibition at 0.022 mM, 50% at 0.020 mM
auranofin
-
competitive, reversible inhibitor of cathepsin B
benzyl N-(3-methoxy-1,2,4-thiadiazolidin-5-yl)-L-alanyl-L-phenylalaninate
IC50: 0.037 mM
benzyl N-([(2R,3R)-3-(butoxycarbonyl)oxiran-2-yl]carbonyl)-L-leucyl-L-prolinate
-
benzyl N-([(2R,3R)-3-(ethoxycarbonyl)aziridin-2-yl]carbonyl)-L-leucinate
-
benzyl N-([(2R,3R)-3-(ethoxycarbonyl)aziridin-2-yl]carbonyl)-L-leucyl-L-prolinate
-
benzyl N-([(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl)-L-leucyl-L-prolinate
-
benzyl N-([(2R,3R)-3-carboxyoxiran-2-yl]carbonyl)-L-leucyl-L-prolinate
-
benzyl N-([(2S,3S)-3-(ethoxycarbonyl)aziridin-2-yl]carbonyl)-L-leucinate
-
benzyl N-([(2S,3S)-3-carboxyoxiran-2-yl]carbonyl)-L-leucyl-L-prolinate
-
benzyl N-[(3-carboxyaziridin-2-yl)carbonyl]-L-leucyl-L-prolinate
-
benzyl [(1R)-1-((1-[hydroxy(3-oxo-2-phenylcycloprop-1-en-1-yl)methyl]-2-methylpropyl)carbamoyl)-2-methylpropyl]carbamate
IC50: 0.000044 mM
benzyl [(1R)-1-((1-[hydroxy(3-oxo-2-phenylcycloprop-1-en-1-yl)methyl]-4-methylpentyl)carbamoyl)-2-methylpropyl]carbamate
IC50: 0.0290 mM
benzyl [(1R)-1-([1-benzyl-2-hydroxy-2-(3-oxo-2-phenylcycloprop-1-en-1-yl)ethyl]carbamoyl)-2-methylpropyl]carbamate
IC50: more than 0.1 mM
benzyl [(1R)-1-([2-hydroxy-1-methyl-2-(3-oxo-2-phenylcycloprop-1-en-1-yl)ethyl]carbamoyl)-2-methylpropyl]carbamate
IC50: 0.0229 mM
benzyl [(1R)-2-((1-[hydroxy(3-oxo-2-phenylcycloprop-1-en-1-yl)methyl]-2-methylpropyl)amino)-1-methyl-2-oxoethyl]carbamate
IC50: 0.00945 mM
benzyl [(1S)-1-((1-[hydroxy(3-oxo-2-phenylcycloprop-1-en-1-yl)methyl]-2-methylpropyl)carbamoyl)-2-methylpropyl]carbamate
IC50: 0.00071 mM
benzylamido-L-trans-epoxysuccinyl-Ile-O-benzyl ester
-
-
benzylamido-L-trans-epoxysuccinyl-Ile-Pro-OH
-
-
benzyloxycarbonyl-Arg-Ser-chloromethylketone
-
-
benzyloxycarbonyl-FA-fmk
-
benzyloxycarbonyl-FGNHO-Bz
-
benzyloxycarbonyl-L-Phe-Ala-fluoromethyl ketone
-
specific inhibitor
benzyloxycarbonyl-L-phenylalanyl-alanine-fluoromethylketone
-
inhibits cathepsin B, treatment stimulates proliferation of type-II pneumocytes and improves degenerative alterations in injured lung occurring with liver injury induced by D-GalN/TNF-alpha, overview
benzyloxycarbonyl-L-phenylalanyl-L-phenylalanyl diazomethyl ketone
irreversible covalent inhibitor
benzyloxycarbonyl-Leu-Leu-Tyr-CHN2
-
-
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
benzyloxycarbonyl-phenylalanyl diazomethyl ketone
irreversible covalent inhibitor
benzyloxycarbonyl-Trp-Met-CHN2
-
-
biotin-NH-(CH2)6-NH-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH
-
selective for cathepsin B over cathepsin L
bis(2-ethyldodecyl) phthalate
-
isolated from seahorse, Hippocampus Kuda Bleeker, NMR structure determination and analysis, overview
bis(2-ethylheptyl) phthalate
-
isolated from seahorse, Hippocampus Kuda Bleeker, NMR structure determination and analysis, overview
Bz-Phe-Arg-CH2F
irreversible covalent inhibitor
BzlNH-tES-Ile-Pro-OBzl
-
-
CA-074-OMe
-
blocks cysteine cathepsins in addition to CatB in in primary human antigen-presenting cells
CA028
irreversible inhibition, IC50: 0.000140 mM
Ca2+
-
40% inhibition at 2 mM
CAA0445
-
noncovalent-type, specific
Cabin-1
-
i.e. LGPVTQE, peptide from human apolipoproteinA-1, 50% inhibition at 0.45 mM
Cabin-2
-
i.e. VLQSSGLYS, peptide from human immunoglobulin G gamma chain, 50% inhibition at 0.5 mM
Cabin-2(1-8)
-
i.e. VLQSSGLY, peptide from human immunoglobulin G gamma chain, 50% inhibition at 0.004 mM
Cabin-3
-
i.e. VVSVLT, peptide from human immunoglobulin G gamma chain, 50% inhibition at 0.02 mM
Cabin-4
-
i.e. LVYDAY, peptide from human transferrin, 50% inhibition at 0.0005 mM
Cabin-A1
-
i.e. SLHTLF, peptide derived from human serum albumin
Cabin-A2
-
i.e. FQNAL, peptide derived from human serum albumin
carbobenzoxy-Phe-NH-CH2CN
-
reversible, 50% inhibition at 0.062 mM
cathepsin B inhibitor III
-
i.e. L-trans.epoxysuccinyl(propylamide)-Ile-Pro or 1-[3-methyl-2-[[3-(propylcarbamoyl)oxirane]-2-carbonyl]amino]pentanoylpyrrolidine-2-carboxylic acid
cathepsin B inhibitor IV
-
i.e. CA074me or methyl 1-[3-methyl-2-[[3-(propylcarbamoyl)oxirane]-2-carbonyl]amino]pentanoylpyrrolidine-2-carboxylate, bone marrow-derived macrophages treated with the cathepsin B-specific chemical inhibitor CA074 methyl ester secret significantly less TNF-alpha than wild-type or nontreated macrophages
cathestatin A
irreversible inhibition, IC50: 0.000260 mM
cathestatin B
irreversible inhibition, IC50: 0.000280 mM
cathestatin C
irreversible inhibition, IC50: 0.000114 mM
CBZ-Phe-Ser(OBzl)-CHN2
cysteine protease inhibitor 1 (CP-1), effective inhibition at 0.05 mM
chagasin
-
an inhibitor from Trypanosoma cruzi, Three residues from chagasin, Leu65, Gly66, and Ala67, interact with cathepsin B residues Gly74, Gly73, and Asn72, binding mode and structure of wild-type enzyme and non-glycosylated S115A and H110A/S115A cathepsin B mutants, modeling, overview
-
chalcone phenyl hydrazone
-
chloro(diethylphenylphosphine)gold(I)
-
-
chloro(ethyldiphenylphosphine)gold(I)
-
-
chloro(triphenylphosphine)gold(I)
-
-
chloro(tris(p-fluorophenyl)phosphine)gold(I)
-
-
chloro-[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
-
-
chloro[2-(1-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl-kN4)phenyl-kC1](pyridine)palladium(1+)
-
-
chloro[2-(1-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl-kN4)phenyl-kC1](triphenylphosphane)palladium(1+)
-
-
chloro[4-(diphenylphosphino-kappaP)benzenamine]gold(I)
-
-
chloro[4-(diphenylphosphino-kappaP)benzoato]gold(I)
-
-
chloro[diphenyl(phenylmethyl)phosphine]gold(I)
-
-
chloro[diphenyl[4-(2-phenyl-1,3-dioxolan-2-yl)phenyl]phosphine-kappaP]gold(I)
-
-
chloro[N-[2-(diphenylphosphino-kappaP)ethyl]benzamide]gold(I)
-
-
chloro[N-[2-(diphenylphosphino-kappaP)ethyl]benzeneacetamide]gold(I)
-
-
chloro[N-[2-(diphenylphosphino-kappaP)ethyl]benzenepropanamide]gold(I)
-
-
chloro[tris(p-methoxyphenyl)phosphine]gold(I)
-
-
chloro[tris(pentafluorophenyl)phosphine]gold(I)
-
-
chloro[[1,1'-biphenyl]-4-yldiphenylphosphine]gold(I)
-
-
CPI-H
-
peptide inhibitor of 13 kDa from rabbit skeletal muscle, noncompetitive
-
CPI-L
-
peptide inhibitor of 23 kDa from rabbit skeletal muscle, noncompetitive
-
CysC
-
natural inhibitor of CatB. CysC deletion in knockout mice leads to an enhanced CatB activity
di-(2-ethylhexyl)phthalate
-
non-competitive inhibitor
diacetato(2-((2dimethylamino)methyl)phenyl)-Au(III)
-
-
diaceto[2-[(2-pyridinyl-kappaN)methyl]-phenyl-kappaC]Au(III)- (SP-4-3)
-
-
dibutyl phthalate
-
non-competitive inhibitor
dichloro(2-((2dimethylamino)methyl)phenyl)Au(III)
-
-
dichloro[2-[(2-pyridinyl-kappaN)methyl]phenyl-kappaC]Au(III)
-
-
EDTA
89% remaining activity at 1 mM, 80% remaining activity at 2 mM
estatin A
irreversible inhibition, IC50: 0.000270 mM
estatin B
irreversible inhibition, IC50: 0.000320 mM
ethoxy-L-trans-epoxysuccinyl-Gly-Pro-OH
-
-
ethoxy-L-trans-epoxysuccinyl-Ile-Ala-OH
-
-
ethoxy-L-trans-epoxysuccinyl-Ile-Ile-OH
-
-
ethoxy-L-trans-epoxysuccinyl-Ile-OH
-
-
ethoxy-L-trans-epoxysuccinyl-Thr-Ile-OH
-
-
ethyl (1R,2S)-2-([(8-hydroxy-5-nitroquinolin-7-yl)methyl]amino)cyclohexane-1-carboxylate
-
-
ethyl (2R,3R)-3-(((1S)-1-[(4-carbamimidamidobutyl)carbamoyl]-3-methylbutyl)carbamoyl)oxirane-2-carboxylate
-
ethyl (2S,3S)-3-(((1S)-3-methyl-1-[(3-methylbutyl)carbamoyl]butyl)carbamoyl)oxirane-2-carboxylate
-
ethyl (2S,3S)-3-(((S)-1-((3-fluorophenethyl)amino)-4-(methylthio)-1-oxobutan-2-yl)carbamoyl)oxirane-2-carboxylate
-
ethyl (2S,3S)-3-(((S)-1-(hexylamino)-4-(methylthio)-1-oxobutan-2-yl)carbamoyl)oxirane-2-carboxylate
-
ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-((3-phenylpropyl)amino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
-
ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-((4-phenylbutyl)-amino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
-
ethyl (2S,3S)-3-(((S)-4-(methylthio)-1-oxo-1-(pentan-3-ylamino)butan-2-yl)carbamoyl)oxirane-2-carboxylate
-
ethyl 1-(5-nitroquinolin-8-yl)piperidine-4-carboxylate
-
-
ethyl 1-[(2R)-2-((1S)-1-(acetyloxy)-2-[((N-[(2,4-difluorophenyl)carbonyl]-L-phenylalanyl)amino)oxy]-2-oxoethyl)pentanoyl]prolinate
IC50: 4.4 mM
ethyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
-
ethyl 4-[(8-hydroxy-5-nitroquinolin-7-yl)methyl]piperazine-1-carboxylate
-
-
EtO-tES-Ile-Pro-OH
-
CA-030
Fe2+
-
79.9% residual activity at 1 mM
Fe3+
-
82.3% residual activity at 1 mM
Fmoc-Tyr-Ala-CHN2
-
FYAD, an irreversible inhibitor of cathepsin B, induces apoptosis of neuroblastoma cells but not of other tumor cells. Inhibitors that affect only one enzyme or fail to maintain inhibition of both cathepsins B and L do not induce apoptosis of these cells, overview
garciniaphenone
-
a prenylated benzophenone isolated from pericarp hexane extract of dried fruits of Rheedia brasiliensis
Gly-Pro-Phe-Pro-Ile
-
amino acids 203-207 of bovine beta-casein, competitive
heparin
-
inhibition is strongly dependent on pH, no inhibition above pH 7.0
HNO
-
from Angeli's salt or induced by LPS and IFN-gamma in RAW macrophages, causes DTT-irreversible inhibition and covalently and permanently inactivation of cathepsin B. Cathepsin B activity is reduced to 53%, 25%, and 57% of maximal activity in nonstimulated, LPS-, and IFN-gamma-treated cells, respectively. Endogenous NO production can provide direct protection for the less reactive protein cysteines by scavenging HNO. Additionally, endogenous cellular production of NO can rescue enzyme function by protective nitrosation of cysteines prior to exposure to HNO
human albutensin A
-
i.e. AFKAWAVAR
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
L-3-trans-(propylcarbamoyl)-oxirane-2-carbonyl-L-isoleucyl-L-proline
-
inhibition of cathepsin B decreases the number of active alpha ENaCs in 2F3 cells
L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl-L-isoleucyl-L-proline
treatment with a cathepsin B inhibitor, leads to transient reduction of local induration, expression of inflammatory cytokines, and subsequent attenuation of the systemic adaptive immune response
L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl-L-isoleucyl-L-proline methyl ester
activity of caspase 3 is significantly reduced in Dengue virus-infected HepG2 cells treated with cathepsin B or S inhibitor. Treatment with cathepsin B inhibitor also reduces the activity of caspase 9
L-3-trans-propylcarbamoyloxirane-2-carbonyl-L-isoleucyl-proline
-
L-tosylphenylalanylchloromethane
-
-
L-trans-epoxysuccinyl-3,5-diiodo-L-tyrosylamido(3-methyl)-butane
-
compound 13b
L-trans-epoxysuccinyl-3,5-diiodo-L-tyrosylamido(3-methyl)-butane ethylester
-
compound 13a
L-trans-epoxysuccinyl-Ile-Pro-methyl ester
-
complete inhibition at 0.025 mM
lipopolysaccharides
-
-
-
malonato(2-((2dimethylamino)methyl)phenyl)Au(III)
-
-
MeO-Gly-Gly-Leu-NH-tES-Leu-Pro-OH
-
NS-134
methoxy-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH
-
selective for cathepsin B over cathepsin L
methyl 3-(4,5-dichloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
-
methyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
-
methyl 3-(5-chloro-4-methyl-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
-
methyl 4-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)butanoate
-
-
methyl 6-(3-(propyldisulfanyl)acrylamido)hexanoate
-
-
methyl N-([(2R,3R)-3-([(1R)-1-([(2S)-2-carboxypyrrolidin-1-yl]carbonyl)-3-methylbutyl]carbamoyl)oxiran-2-yl]carbonyl)-L-leucylglycylglycinate
-
methyl N-([(2S,3S)-3-([(1R)-1-([(2S)-2-carboxypyrrolidin-1-yl]carbonyl)-3-methylbutyl]carbamoyl)oxiran-2-yl]carbonyl)-L-leucylglycylglycinate
-
Miraziridine A
irreversible covalent inhibitor
mizaridine
IC50: 0.00205 mM
N,N-dimethyl-1-(5-nitroquinolin-8-yl)piperidine-3-carboxamide
-
-
N-(((2R,3R)-3-[(1-methylethyl)carbamoyl]oxiran-2-yl)carbonyl)-L-leucyl-L-proline
-
N-(((2S,3S)-3-[(1-methylethyl)carbamoyl]oxiran-2-yl)carbonyl)-L-leucyl-L-proline
-
N-((1S)-2-[(2R,3R)-2-[(benzyloxy)carbonyl]-3-(ethoxycarbonyl)aziridin-1-yl]-1-methyl-2-oxoethyl)-Na-(tert-butoxycarbonyl)-L-phenylalaninamide
-
N-(1-cyanocyclopropyl)-8-hydroxy-5-nitroquinoline-7-carboxamide
-
N-(3-carboxy-1,2,4-thiadiazolidin-5-yl)-L-leucyl-L-proline
IC50: 0.300 mM
N-(3-methoxy-1,2,4-thiadiazolidin-5-yl)-L-leucyl-L-proline
IC50: 0.0026 mM
N-(3-methyl-1,2,4-thiadiazolidin-5-yl)-L-leucyl-L-proline
IC50: 0.447 mM
N-(3-phenyl-1,2,4-thiadiazolidin-5-yl)-L-leucyl-L-proline
IC50: 0.074 mM
N-(cyanomethyl)-5-nitroquinoline-8-carboxamide
-
N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide
-
N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide
-
N-(L-3-trans-carboxyoxirane-2-carbonyl)-Ile-Pro
-
CA-030
N-(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucylamino-3-methylbutane
-
E64c
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-Ile-Pro
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
N-(trans-epoxysuccinyl)-L-leucine 4-guanidinobutylamide
addition of E-64 significantly decreases the activities of cathepsin B and caspase 3, and TUNEL-positive cells in heat-shocked in vitro maturated (IVM) bovine cumulus-oocyte complexes. Addition of inhibitor during in vitro maturation under heat shock conditions significantly improves both developmental competence and quality of the produced embryos
N-([(2R,3R)-1-[N-(tert-butoxycarbonyl)-L-phenylalanyl]-3-(ethoxycarbonyl)aziridin-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2R,3R)-3-((5-amino-1-[(4-carbamimidamidobutyl)carbamoyl]pentyl)carbamoyl)oxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2R,3R)-3-(butoxycarbonyl)oxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl)-L-leucyl-L-arginine
-
N-([(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2R,3R)-3-([(1R)-1-([(2S)-2-carboxypyrrolidin-1-yl]carbonyl)-3-methylbutyl]carbamoyl)oxiran-2-yl]carbonyl)-L-leucylglycyl-N-(6-[((2-[6-(diethylamino)-3-(diethyliminio)-3H-xanthen-9-yl]phenyl)carbonyl)amino]hexyl)glycinamide
-
N-([(2R,3R)-3-([(1R)-1-([(2S)-2-carboxypyrrolidin-1-yl]carbonyl)-3-methylbutyl]carbamoyl)oxiran-2-yl]carbonyl)-L-leucylglycyl-N-[6-((5-[(4R)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl)amino)hexyl]glycinamide
-
N-([(2R,3R)-3-carboxyoxiran-2-yl]carbonyl)-L-leucyl-L-arginine
-
N-([(2R,3R)-3-carboxyoxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2S,3S)-1-[N-(tert-butoxycarbonyl)-L-phenylalanyl]-3-(ethoxycarbonyl)aziridin-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2S,3S)-3-((5-amino-1-[(4-carbamimidamidobutyl)carbamoyl]pentyl)carbamoyl)oxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2S,3S)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-([(2S,3S)-3-carboxyoxiran-2-yl]carbonyl)-L-leucyl-L-leucine
-
N-([(2S,3S)-3-carboxyoxiran-2-yl]carbonyl)-L-leucyl-L-proline
-
N-acetyl-3,5-diphenyl pyrazolines
-
N-acetyl-5-(4-bromophenyl)-3-phenyl-2-pyrazoline
-
N-acetyl-5-(4-chlorophenyl)-3-phenyl-2-pyrazoline
-
N-acetyl-5-(4-methoxyphenyl)-3-phenyl-2-pyrazoline
-
N-acetyl-5-(4-methylphenyl)-3-phenyl-2-pyrazoline
-
N-acetyl-5-(4-nitrophenyl)-3-phenyl-2-pyrazoline
-
N-Acetyl-Leu-Leu-methional
reversible inhibitor
N-alpha-[(benzyloxy)carbonyl]-N-[(3S)-1-[(2,6-dimethylbenzoyl)oxy]-7-[(6-[(2Z)-2-[(2E,4E)-5-(1-ethyl-3,3-dimethyl-5-sulfo-3H-indolium-2-yl)penta-2,4-dien-1-ylidene]-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]-2-oxoheptan-3-yl]-L-phenylalaninamide
-
N-benzoyl-3,5-diphenylpyrazoline
-
N-benzoyl-5-(2-chloro phenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(2-methoxyphenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(2-nitrophenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(3-chloro phenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(3-methoxy phenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(3-nitrophenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(4-chloro phenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(4-methoxy phenyl)-3-phenylpyrazoline
-
N-benzoyl-5-(4-nitrophenyl)-3-phenylpyrazoline
-
N-benzyl-5-nitroquinolin-8-amine
-
-
N-benzyl-N,N-diethylethanaminium 1-trichloro-4-chloro-2,3-dihydro-2-oxatellurophene
-
-
N-benzyl-N,N-diethylethanaminium 2,2,2,4-tetrachloro-2,5-dihydro-2lambda6-[1,2]-oxatellurolinate complex
-
N-benzyl-N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide
-
N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-2-carboxamide
-
N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide
-
N-benzyl-N-methyl-5-nitroquinolin-8-amine
-
-
N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone
N-chloroacetyl-Gly-Leu-OH
-
N-chloroacetyl-Leu-Leu-OH
-
N-chloroacetyl-Leu-Leu-OMe
-
N-chloroacetyl-Lys-Leu-OH
-
N-chloroacetyl-Phe-Leu-OH
-
N-chloroacetyl-Phe-Met-OH
-
N-chloroacetyl-Ser-Leu-OH
-
N-formyl-3,5-diphenylpyrazoline
-
N-formyl-5-(2-chlorophenyl)-3-phenylpyrazoline
-
N-formyl-5-(2-methoxyphenyl)-3-phenylpyrazoline
-
N-formyl-5-(2-nitrophenyl)-3-phenylpyrazoline
-
N-formyl-5-(3-chlorophenyl)-3-phenylpyrazoline
-
N-formyl-5-(3-methoxyphenyl)-3-phenylpyrazoline
-
N-formyl-5-(3-nitrophenyl)-3-phenylpyrazoline
-
N-formyl-5-(4-chlorophenyl)-3-phenylpyrazoline
-
N-formyl-5-(4-methoxyphenyl)-3-phenylpyrazoline
-
N-formyl-5-(4-nitrophenyl)-3-phenylpyrazoline
-
N-p-tosylphenyl-L-lysine-chloromethane
-
-
N-phenyl-3-(propyldisulfanyl)-3-chloro-acrylamide
-
-
N-phenyl-3-(propyldisulfanyl)acrylamide
-
-
n-propyl-(2S,3S)-trans-epoxysuccinyl-L-Ile-OH
kinetic analysis
N-tosyl-lysyl chloromethylketone
N-tosyl-phenylalanine chloromethylketone
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
N-[(1R)-1-cyano-2-([3-(2H-tetrazol-2-yl)benzyl]oxy)ethyl]-3-methyl-Na-(3-oxo-1,3-dihydro-2-benzofuran-5-yl)-L-phenylalaninamide
IC50: 0.000005 mM
N-[(1S)-3-(benzyloxy)-1-cyanopropyl]-Nalpha-(diphenylacetyl)-3-methyl-L-phenylalaninamide
IC50: 0.0000102 mM
N-[(3-methoxy-1,2,4-thiadiazolidin-5-yl)carbamoyl]-L-leucyl-L-proline
IC50: 0.390 mM
N-[2-[(3-carboxyphenyl)methoxy]-1-(S)-cyanoethyl]-3-methyl-Nalpha-(2,4-difluorobenzoyl)-L-phenylalaninamide
-
50% inhibition at 6.8 nM, selective for cathepsin B
N-[[1-(1,3-benzothiazol-2-yl)piperidin-3-yl]methyl]-8-hydroxy-5-nitroquinoline-7-carboxamide
-
N-[[1-(1,3-benzoxazol-2-yl)piperidin-3-yl]methyl]-8-hydroxy-5-nitroquinoline-7-carboxamide
-
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
Na-[(benzyloxy)carbonyl]-N-(3-methoxy-1,2,4-thiadiazolidin-5-yl)-L-phenylalaninamide
IC50: 0.021 mM
Nalpha-(tert-butoxycarbonyl)-N-((1S)-2-[(2R,3R)-2-carboxy-3-(ethoxycarbonyl)aziridin-1-yl]-1-methyl-2-oxoethyl)-L-phenylalaninamide
-
Nalpha-[(benzyloxy)carbonyl]-N-[(2R,3S)-2-(carboxyoxy)-4-oxoazetidin-3-yl]-L-phenylalaninamide
IC50: 0.00047 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(3S,4R)-2-oxo-4-phenoxyazetidin-3-yl]-L-phenylalaninamide
IC50: 0.00043 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(5R,6R)-4,4-dioxido-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6-yl]-L-phenylalaninamide
IC50: 0.00035 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(5R,6R)-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6-yl]-L-phenylalaninamide
IC50: more than 0.00050 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(5R,6S)-7-oxo-4-oxa-1-azabicyclo[3.2.0]hept-6-yl]-L-phenylalaninamide
IC50: 0.00176 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(6R)-4-oxido-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6-yl]-L-phenylalaninamide
IC50: 0.0164 mM
NAMI-A
-
i.e. [imidazoleH][trans-Ru(DMSO)(imidazole)Cl4], an antimetastatic compound
-
Ni2+
-
26.7% residual activity at 1 mM
oryzacystatin-1 clone A10
-
-
-
Os(II)-pentamethylcyclopentadienyl 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane N-acetyl-L-cysteine-N'-methylamide
-
i.e. OSPTAC
-
oxalo-RAPTA
-
ruthenium(II)-arene compound
oxidized glutathione
-
concentrations above10 mM significantly decrease activity
p-chloromercuriphenyl sulfonic acid
p-hydroxymercuribenzoate
-
-
Pefabloc SC
1.0 mM, 11% loss of activity
penetratin HP-CO-(CH2)5-NH-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH
-
selective for cathepsin B over cathepsin L, penetratin moiety allows penetration of cell membrane, almost complete inactivation at 300 nM, at 10 nM block of about 60% of intracellular enzyme activity
Peptidyl chloromethylketones
-
-
peptidyl cyclopropenone
reversible inhibitor
-
peptidyl diazomethyl ketone derivatives
-
phenylacetyl hydrazine
competitive inhibition
phenylmethanesulfonyl fluoride
phenylmethylsulfonyl fluoride
-
62.8% residual activity at 1 mM
PrnNH-tES-Ile-Pro-OBzl
-
-
PrnNH-tES-Ile-Pro-OH
-
CA-074
PrnNH-tES-Ile-Pro-OMe
-
-
Pro-Phe-Pr-Gly-Pro-Ile
-
amino acids 61-66 of bovine beta-casein, competitive
propylcarbonyl-L-trans-epoxysuccinyl-Ile-O-benzyl ester
-
-
propylcarbonyl-L-trans-epoxysuccinyl-Ile-Pro-O-methyl ester
-
-
PRT2005
-
commercial peptidyl ketone inhibitors, Prototek, 50% inhibition at less than 0.001 mM
-
PRT2253
-
commercial peptidyl ketone inhibitors, Prototek, 50% inhibition at less than 0.001 mM
-
RAPTA-BC
-
ruthenium(II)-arene compound
RAPTA-BI
-
ruthenium(II)-arene compound
RAPTA-C
-
i.e. carbo-RAPTA, ruthenium(II)-arene compound
RAPTA-H
-
ruthenium(II)-arene compound
-
RAPTA-Me+C
-
ruthenium(II)-arene compound
RAPTA-NH3
-
ruthenium(II)-arene compound
RAPTA-OH
-
ruthenium(II)-arene compound
RAPTA-pentaOH
-
binding structure from cyrstal structure of the inhibitor bound to cathepsin B, overview
RAPTA-T
-
ruthenium(II)-arene compound
RAPTA-TBMe
-
ruthenium(II)-arene compound
RAPTA-TBOH
-
ruthenium(II)-arene compound
rhodamine B-NH-(CH2)6-NH-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH
-
selective for cathepsin B over cathepsin L
RNA interference oligonucleotide shRNA-CTSB2
most efficient inhibition of cathepsin B at both mRNA and protein levels and results in suppressing endometrial cancer growth and development in vivo
-
Ru(II)-pentamethylcyclopentadienyl 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane N-acetyl-L-cysteine-N'-methylamide
-
i.e. RAPTA-C
-
sodium chloro[[4,4',4''-(phosphinidyne-kappaP)tris[benzenesulfonato]]aurate]
-
-
Soybean trypsin inhibitor
-
51.2% residual activity at 0.1 g/l
-
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
-
-
TMC-52A
irreversible inhibition, IC50: 0.000320 mM
TMC-52B
irreversible inhibition, IC50: 0.000200 mM
TMC-52C
irreversible inhibition, IC50: 0.000460 mM
TMC-52D
irreversible inhibition, IC50: 0.000280 mM
tokaramide A
IC50: 0.0000624 mM
TPCK
0.2 mM, partial inhibition; 0.2 mM, partial inhibition; 0.2 mM, partial inhibition; 0.2 mM, partial inhibition
trans-cis-cis-[RuCl2(DMSO)2(2-amino-5-methyl-thiazole)2]
-
i.e. (PMRu52), a ruthenium(II) compound acting as a strong inhibitor of cathepsin B, crystal structure and binding structure analysis, overview
trans-epoxysuccinyl-L-leucyl-amido(4-guanidino)butane
trans-epoxysuccinyl-L-leucyl-smido(4-guanidino)butane
E-64
trans-epoxysuccinyl-leucylamido(4-guanidino)butane
trichloro(dioxoethylene-O,O')tellurate
-
-
triethylphosphine(2,3,4,6-tetra-O-acetyl-beta-1-D-thiopyranosato-S)gold(I)
-
auranofin
Trp
inactivation rate is 12 mM/min
Tyr-(O-methyl)
inactivation rate is 1.548 mM/min
Tyr-(O-tert-butyl)
inactivation rate is 0.618 mM/min
Urea
-
inactivated at 3 M
WF14861
irreversible inhibition, IC50: 0.000016 mM
WF14865A
irreversible inhibition, IC50: 0.0000084 mM
WF14865B
irreversible inhibition, IC50: 0.000013 mM
wortmannilactone E
-
i.e. (19S)-(4S,7R)-7-[(1E,3E,5E,7E)-8-[(2S,5S,6S)-5,6-dihydro-5-hydroxy-3,5,6-trimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-4,6,7-trimethyl-2-oxabicyclo[2.2.1]heptane-3,5-dione, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, Yunnan Province, China. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview
wortmannilactone F
-
i.e. (19R)-(4S,7R)-7-[(1E,3E,5E,7E)-8-[(2S,5R,6S)-5,6-dihydro-5-hydroxy-3,5,6-trimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-4,6,7-trimethyl-2-oxabicyclo[2.2.1]heptane-3,5-dione, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, Yunnan Province, China. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview
wortmannilactone G
-
i.e. methyl (2R)-2-[(3R,4R)-3-[(1E,3E,5E,7E)-8-[(2S,3R,6S)-3,6-dihydro-3-hydroxy-3,5,6-trimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-3,4-dimethyl-5-oxotetrahydrofuran-2-yl]propanoate, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, Yunnan Province, China. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview
wortmannilactone H
-
i.e. (4S,7R)-7-[(1E,3E,5E,7E)-8-[(2S,3R,6S)-3,6-dihydro-3-hydroxy-3,6-dimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-4,6,7-trimethyl-2-oxabicyclo[2.2.1]heptane-3,5-dione, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, in Chinas Yunnan Province. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview
YM 51084
IC50: 0.000012 mM
Z-Arg-Gly-Pro-Agly-Gly-Glu-OMe
-
Z-Arg-Leu-Arg-alpha-aza-glycyl-Ile-Val-OMe
-
i.e. ZRLR, a highly selective cathepsin B inhibitor, cell-permeable, almost complete inhibition at 0.0001 mM
Z-Arg-Leu-His-Agly-Ile-Val-OMe
-
Z-Arg-Leu-Phe-Agly-Val-Ala-OMe
-
Z-Arg-Leu-Val-Agly-Gly-Asp-OMe
-
Z-Arg-Leu-Val-Agly-Gly-Glu-OMe
-
Z-Arg-Leu-Val-Agly-Ser-Ala-OMe
-
Z-Arg-Nle-Pro-Agly-Gly-Glu-OMe
-
Z-Arg-Nle-Val-Agly-Gly-Glu-OMe
-
Z-Phe-Ala-CH2-O-CO-(2,4,6-trimethyl)-Ph
-
Z-Phe-Ala-CH2-O-CO-(2,5-(CF3)2)-Ph
-
Z-Phe-Ala-CH2-O-CO-(2,6-(CF3)2)-Ph
-
Z-Phe-Cys(SBzl)-CH2-O-CO-(2,6-(CF3)2)-Phe
-
Z-Phe-Gly-NHO-Bz
-
an inhibitor of both cathepsins B and L, causes death of many cell types
Z-Phe-Lys-CH2-O-CO-(2,4,6-trimethyl)-Ph
-
[(1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one)PdCl]2
-
-
[(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
-
-
[(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)Pd(1,3,5-triaza-7-phosphoadamantane)Cl]
-
-
[(benzyl(methyl)sulfane)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
[(N,N-dimethyl-1-phenylmethanamine)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
-
-
[(N,N-dimethyl-1-phenylmethanamine)Pd(1,3,5-triaza-7-phosphoadamantane)Cl]
-
-
[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
-
-
[2-(1-benzyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl-kN4)phenyl-kC1](chloro)(pyridine)palladium(1+)
-
-
[2-(1-benzyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-5-yl-kN4)phenyl-kC1](chloro)(triphenylphosphane)palladium(1+)
-
-
[2-(mercapto-kappaS)benzoato(2-)-kappaO][2-[(2-pyridinyl-kappaN)methyl]phenyl-kappaC]Au(III)
-
-
[2-[2-(2,4-dioxo-1,3-thiazolidin-3-yl)ethylamino]-2-oxoethyl] 2-(furan-2-carbonylamino) acetate
-
i.e. DOFA, a reversible, double-headed competitive inhibitor of cathepsin B, the dioxothiazolidine head of the compound sterically hinders binding of the C-terminal residue of substrates resulting in inhibition of the exopeptidase activity of cathepsin B in a physiopathologically relevant pH range, competitive versus substrates ortho-aminobenzoyl-Gly-Ile-Val-Arg-Ala-Lys-Nepsilon-2,4-dinitrophenyl-OH and carbobenzoxy-Arg-Arg-7-amido-4-methylcoumarin, structure and enzyme docking, overview
[imidazoleH][trans-Ru(imidazole)2Cl4]
-
i.e. KP1019
-
[Ir(III)-pentamethylcyclopentadienyl-(1,3,5-triaza-7-phospatatricyclo[3.3.1.1]decane)Cl2]
-
-
-
[Ir(III)-pentamethylcyclopentadienyl-(1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane)2Cl]PF6
-
-
-
[Ir(III)-pentamethylcyclopentadienyl-methyl(1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane)Cl2]OTf
-
-
-
[Ir(III)-pentamethylcyclopentadienyl-methyl(1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane)Cl](OTf)PF6
-
-
-
[L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline
-
-
[L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline methyl ester
-
CA-074-Me, specific inhibitor
[N-(L-3-trans-propylcarbamoyl oxirane-2-carbonyl)-L-isoleucyl-L-proline]
-
specific inhibitor
[N-benzyl-N,N-diethylethanaminium]2 hexachloro-lambda6-tellane
-
-
[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
[Pd2((S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
[Pd2(1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one)2(m-1,2-ethanebis(diphenylphosphine))Cl2]
-
structure analysis by NMR spectroscopy and in the solid state by X-ray crystallography; structure analysis by NMR spectroscopy and in the solid state by X-ray crystallography. It inhibits cathepsin B, and also K562 leukemia cells with an IC50 value of 0.0043 mM after 1 h exposure
[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
[Ru(II)-pentamethylcyclopentadienyl-(1,3,5-triaza-7-phosphatatricyclo[3.3.1.1]decane)Cl2]
-
-
-
(2Z)-1,3-bis(2-methoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
(2Z)-1,3-bis(2-methoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
-
1,10-phenanthroline
-
77.3% residual activity at 1 mM
1,10-phenanthroline
66% remaining activity at 1 mM, 68% remaining activity at 2 mM
1-tosylamide-2-phenylethyl chloromethylketone
-
moderate effect
1-tosylamide-2-phenylethyl chloromethylketone
-
-
1-tosylamide-2-phenylethyl chloromethylketone
-
-
1-tosylamide-2-phenylethyl chloromethylketone
-
-
2,2'-dipyridyl disulfide
-
-
2,2'-dipyridyl disulfide
-
-
2,2'-dipyridyl disulfide
-
-
acetyl-YVAD-chloromethyl ketone
-
caspase inhibitor, inhibition of enzyme contributes to neuroprotective properties of the inhibitor
acetyl-YVAD-chloromethyl ketone
-
caspase inhibitor, inhibition of enzyme contributes to neuroprotective properties of the inhibitor
antipain
-
complete inhibition at 1 mM
antipain
-
93% inhibition at 1 microM
bafilomycin A1
-
bafilomycin A1
-
100 nM significantly inhibits activity
CA-074
-
-
CA-074
a cathepsin B-specific inhibitor, inhibition CmCatB1
CA-074
irreversible cathepsin B inhibitor
CA-074
-
a selective cell-impermeable cathepsin B inhibitor
CA-074
-
a cathepsin B inhibitor
CA-074
-
a cathepsin B inhibitor significantly attenuates the ratio of hypodiploid and apoptotic cells, partially blocks caspase 3 activation and inhibits reduction of cell viability induced by emodin
CA-074
-
cathepsin B inhibitor III, i.e. [L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline
CA-074
i.-e. [L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline and its derivates, irreversible covalent inhibitor
CA-074
-
specific inhibitor
CA-074
irreversible cathepsin B inhibitor
CA-074
-
cathepsin B-specific inhibitor
CA-074
0.01 mM, 97% loss of activity
CA-074 Me
-
CA-074 Me
99.4% inhibition at 0.010 mM in cell lysates
CA-074 Me
-
a specific cathepsin B inhibitor
Ca-074 methyl ester
0.001 mM, complete inhibition; 0.001 mM, complete inhibition; 0.001 mM, complete inhibition; 0.001 mM, complete inhibition
CA-074-Me
-
CA-074-Me
-
Cat B-selective inhibitor
CA-074-Me
-
suppresses microglia conditioned culture medium-induced glioma cell death
CA-074-Me
-
strong inhibition
CA-074-Me
-
i.e. propylcarbonyl-L-trans-epoxysuccinyl-Ile-Pro-OH, enzyme binding structure at the active site cleft, modelling, overview
CA-074-Me
-
cathepsin B inhibition decreases hepatic stellate cell proliferation and the expression of phenotypic markers of hepatic stellate cell activation, and it down-regulate alpha-smooth musle actin mRNA and protein levels in LX2 cells, overview. Reduction of CtsB and/or CtsD levels by siRNA decreases cell proliferation, compared to control siRNA-transfected LX2 cells
CA-074-Me
-
i.e. [L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline methyl ester
CA-074-Me
-
in vivo inhibition
CA-074-Me
-
CA-074Me clearly inhibits cath-B expression in the subcutaneous heteroplastic pancreatic carcinoma model, and demonstrates an anti-neoplastic and anti-angiogenesis effect, overview
CA-074-Me
-
a specific inhibitor, inhibits pro-interleukin-1beta processing in microglia
CA-074-Me
-
a potent and specific CtsB inhibitor, CtsB inhibition blunts AKT phosphorylation in activated hepatic stellate cells in response to platelet-derived growth factor
CA-074-Me
-
cathepsin B inhibitor IV. Inhibition of cathepsin B blocks MEK1 cleavage induced by anthrax lethal toxin through delaying LeTx release into the cytoplasm. The cathepsin B inhibitor prevents cell death induced by anthrax lethal toxin in RAW 264.7 macrophages
CA-074-Me
-
i.e. [L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline methyl ester
CA-074-Me
-
suppresses microglia conditioned culture medium-induced glioma cell death
CA-074Me
-
-
CA-074Me
-
a specific inhibitor for cathepsin B
CA-074Me
-
a selective cell-permeable cathepsin B inhibitor
CA-074Me
-
cathepsin B specific inhibitor, cathepsin B inhibitor IV, i.e. [L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl]-L-isoleucyl-L-proline methyl ester
CA-074Me
-
a cathepsin B inhibitor
CA030
irreversible inhibition, IC50: 0.00000438 mM
CA030
-
i.e. ethoxy-L-trans-epoxysuccinyl-Ile-Pro-OH
CA074
-
-
CA074
-
high specificity, 34000fold more effective on enzyme than on cathepsin X
CA074
irreversible inhibition, IC50: 0.00000194 mM
CA074
treatment of colorectal cancer cells cells with the cathepsin B inhibitor Ca074 leads to invasiveness of human CRC cells
CA074
-
an irreversible CB inhibitor
CA074Me
-
-
CA074Me
-
cathepsin B specific inhibitor
CA074Me
-
inhibition affects myotube size and number, fusion-related creatine phosphokinase activity and myosin heavy chain protein, inhibition occurs at each stage of differentiation
chicken cystatin
-
-
Chloroquine
-
-
chymostatin
-
80% inhibition at 6 microM
chymostatin
-
85% inhibition at 5 microM
chymostatin
0.1 mM, 96% loss of activity
Cu2+
-
32% residual activity at 1 mM
cystatin
-
the enzyme retains 10% and 5% of its initial activity, after 30 min of incubation at 37°C, in the presence of 75 and 100 nM recombinant cystatin, respectively
-
cystatin
binding sequence is FFEYDGVVSGGPYLGK, by mass spectrometric analysis
-
cystatin
-
poor inhibitor, 51% inhibition at 100 nM
-
cystatin C
-
-
cystatin C
-
Porphyromonas gingivalis interrupts the interaction of cathepsin B with its inhibitor cystatin
-
cystatin C
-
an endogenous inhibitor of cysteine cathepsins, expression patterns of cathepsin B and cystatin C
-
cystatin C
-
CysC or CST3, an endogenous inhibitor of cysteine proteases, including cathepsin B
-
cystatin C
-
an endogenous inhibitor of cysteine cathepsins, expression patterns of cathepsin B and cystatin C
-
DCG-04
-
an E-64-type inhibitor, inhibits both mature cathepsin B and its zymogen
E-64
-
complete inhibition at 1 mM
E-64
-
inhibition of cathepsin B greatly improves the developmental competence of bovine oocytes and increases the number of high-quality embryos, overview
E-64
a cysteine protease inhibitor, inhibition of CmCatB1
E-64
0.02 mM, complete inhibition; 0.02 mM, complete inhibition; 0.02 mM, complete inhibition; 0.02 mM, complete inhibition
E-64
-
an irreversible cysteine protease inhibitor
E-64
irreversible inhibition, IC50: 0.000055 mM
E-64
-
irreversible inhibitor
E-64
-
broad-spectrum cysteine protease inhibitor, complete inhibition
E-64
-
an irreversible cysteine protease inhibitor
E-64
irreversible covalent inhibitor
E-64
-
i.e. L-trans-epoxysuccinyl-leucylamido-(4-guanidino)-butane, irreversible inhibitor
E-64
-
a broad cysteine protease inhibitor
E-64
0.01 mM, 99% loss of activity
E-64c
irreversible inhibition, IC50: 0.00000870 mM
E-64c
inhibition of Cathepsin B alone not only reduces hyperthermic injury-induced apoptosis significantly but enhances the beneficial effects of preinduction of HSP-70 in reducing hyperthermic injury-induced apoptosis in H9C2 cells significantly
E-64d
-
E-64d
-
i.e. (L-3-trans-ethoxycarbonyloxirane-2-carbonyl)-L-leucine(3-methylbutyl)amide
E64
-
E64
-
kinetics, pH-dependence of inhibition
E64c
-
-
E64c
-
the (2S,3S)-3-(L-[N-(3-methylbutyl)amino]leucyl) side chain binds at the S1 and S3 subsites
E64d
substituting ethyl(methyl) sulfane for 2-methylbutane (R2) of E64d improves the inhibitory activity and selectivity for cathepsin B inhibition
E64d
i.e. loxistatin, irreversible covalent inhibitor
Elastatinal
-
-
Hg2+
-
-
human cystatin A
-
-
-
Human cystatin C
-
-
-
iodoacetamide
-
-
iodoacetamide
-
concentrations above10 mM significantly decrease activity
iodoacetic acid
-
complete inhibition at 1 mM
iodoacetic acid
0.01 mM, partial inhibition; 0.01 mM, partial inhibition; 0.01 mM, partial inhibition; 0.01 mM, partial inhibition
iodoacetic acid
-
100% inhibition at 0.5 mM
iodoacetic acid
-
complete inhibition at 1 mM
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
L-3-carboxy-2,3-trans-epoxypropionyl-leucylamido-(4-guanidino)butane
-
E-64
leupeptin
-
42.5% residual activity at 0.1 mM
leupeptin
-
98% inhibition at 1 microM
leupeptin
IC50: 0.0000213 mM
leupeptin
leupeptin lacks selectivity since it inhibits both serine and cysteine proteases
leupeptin
-
Ki: 0.15-0.17 nM
leupeptin
4% remaining activity at 0.010 mM, 1% remaining activity at 0.1 mM
Mg2+
-
-
Mg2+
-
50% inhibition at 2 mM
Mn2+
-
85.4% residual activity at 1 mM
Mn2+
-
10% inhibition at 8 mM, no inhibition at 2 mM
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-Ile-Pro
-
CA-074
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-Ile-Pro
-
CA-074
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline
CA-074, 40.4% inhibition at 0.010 mM in cell lysates
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline
CA-074
N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline
CA-074; CA-074; CA-074; CA-074
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline
-
i.e. CA074, a cathepsin B-selective inhibitor
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline
-
i.e. CA074
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
i.e. CA074Me, inhibits the enzyme and PANC-1 cellular invasiveness, overview
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
-
i.e. CA074Me, a cathepsin B-selective inhibitor
N-(L-3-trans-propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
-
i.e. CA074Me
N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone
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N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone
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N-ethylmaleimide
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no inhibition at 1 mM
N-ethylmaleimide
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no inhibition at 1 mM
N-ethylmaleimide
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concentrations above10 mM significantly decrease activity
N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-lysyl chloromethylketone
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N-tosyl-phenylalanine chloromethylketone
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N-tosyl-phenylalanine chloromethylketone
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N-tosyl-phenylalanine chloromethylketone
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NC-2300
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i.e. monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate, a cysteine cathepsin inhibitor
NC-2300
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i.e. monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate, a cysteine cathepsin inhibitor
p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuriphenyl sulfonic acid
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p-chloromercuriphenyl sulfonic acid
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peptidyl diazomethyl ketone derivatives
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peptidyl diazomethyl ketone derivatives
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peptidyl diazomethanes
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phenylmethanesulfonyl fluoride
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no inhibition at 10 microM
phenylmethanesulfonyl fluoride
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no inhibition at 0.1 mM
phenylmethanesulfonyl fluoride
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27-33% inhibition at 0.5 mM
phenylmethanesulfonyl fluoride
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27-33% inhibition at 0.5 mM
phenylmethanesulfonyl fluoride
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18% inhibition in the presence of 10 microM
phenylmethanesulfonyl fluoride
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no inhibition at 0.5 mM
PMSF
2 mM, partial inhibition; 2 mM, partial inhibition; 2 mM, partial inhibition; 2 mM, partial inhibition
PMSF
98% remaining activity at 0.5 mM, 93% remaining activity at 1 mM
Proteinase inhibitors
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from chicken´s egg white
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Proteinase inhibitors
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from potato tuber
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Proteinase inhibitors
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from rat, human, tuna fish, toad, chicken
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sheep cystatin B
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trans-epoxysuccinyl-L-leucyl-amido(4-guanidino)butane
E-64
trans-epoxysuccinyl-L-leucyl-amido(4-guanidino)butane
E-64, 63.2% inhibition at 0.010 mM in cell lysates
trans-epoxysuccinyl-L-leucyl-amido(4-guanidino)butane
E-64; E-64; E-64
trans-epoxysuccinyl-L-leucyl-amido(4-guanidino)butane
E-64, 43% remaining activity at 0.005 mM, 32% remaining activity at 0.020 mM, 2% remaining activity at 0.030 mM
trans-epoxysuccinyl-leucylamido(4-guanidino)butane
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trans-epoxysuccinyl-leucylamido(4-guanidino)butane
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Zn2+
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14.7% residual activity at 1 mM
Zn2+
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80% inhibition at 2 mM
[(benzyl(methyl)sulfane)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
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[(benzyl(methyl)sulfane)Pd(1,3,5-triaza-7-phosphaadamantane)Cl]
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[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
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[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
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[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
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[Pd2((R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
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[Pd2((S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
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[Pd2((S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
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[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
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[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,1'-bis(diphenylphosphino)ferrocene)Cl2]
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[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
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[Pd2(1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one)2(m-1,2-bis(diphenylphosphino)ethane)Cl2]
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additional information
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not inhibited by dithiothreitol, L-cysteine, EDTA, and EGTA
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additional information
no inhibition with N-chloroacetyl-Gly-Gly-OH
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additional information
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no inhibition with N-chloroacetyl-Gly-Gly-OH
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additional information
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inhibitor screening and docking studies to cathepsin B, overview. Predicted bioactivities of inhibitor candidates and molecular mechanics
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additional information
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inhibition of cathepsin B by antitumor ruthenium(II)-arene compounds, mechanisms of binding/inhibition, overview
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additional information
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isolation and identification of a protein inhibitor of cathepsin B from Pseudomonas sp. strain PB01, phylogenetic distribution in Pseudomonas species, overview
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additional information
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correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles, that show in vitro activity as cytotoxic agents on A2780/S cells and also as cathepsin B inhibitors, synthesis and crystal structure of palladacycles, overview
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additional information
no inhibition of CmCatB1 by PMSF, leupeptin, pepstatin A, ethanol and DMSO
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additional information
no inhibition of CmCatB1 by PMSF, leupeptin, pepstatin A, ethanol and DMSO
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additional information
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no inhibition of CmCatB1 by PMSF, leupeptin, pepstatin A, ethanol and DMSO
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additional information
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no inhibition of CatB by soybean cysteine protease inhibitor
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additional information
No effects on cathepsin B activity by human chorionic gonadotropin and 17beta-estradiol
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additional information
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No effects on cathepsin B activity by human chorionic gonadotropin and 17beta-estradiol
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additional information
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analysis of further dipeptidyl nitriles as selective inhibitors
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additional information
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ruthenium(II)-arene compounds behave as powerful inhibitors
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additional information
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inhibitory activities of N-cyano-tetrahydro-pyridazine derivatives, docking studies, overview
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additional information
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inhibitor screening, overview
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additional information
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alpha-1-antitrypsin aerosolised augmentation abrogates neutrophil elastase-induced expression of cathepsin B in vivo and in vitro
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additional information
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design and synthesis of hypervalent tellurium compounds, and irreversible inhibition of cathepsins B by hypervalent tellurium compounds, e.g. organotellurium(IV) compounds, i.e. organotelluranes, that react with thiols forming mixed dichalcogenides, with a tellurium-sulfur bond. Mechanisms for two- and one-step irreversible enzyme inhibition, overview
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additional information
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no inhibition of cathepsin B by SDF-1 in vivo
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additional information
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95-100% enzyme inhibition is required to cause neuroblastoma cell death
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additional information
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development of cathepsin inhibitors and structure-based design of cathepsin B-specific inhibitor, binding mode at the active site and structure-activity relationship, overview. Quantitative assesment of inhibitor binding at the SN-site of cathepsin B, overview
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additional information
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screening of pyrimidotriazine-diones and pyrazole sulfonamides as cathepsin B inhibitors, structure-function relationship, overview. Pyrimidotriazine-dione inhibitors, along with several structurally unrelated compounds, are inactive in presence of the reductant cysteine or DTT, thus the inhibitors are acting through a DTT-dependent redox cycling mechanism, rather than through direct inhibition of the enzyme
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additional information
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correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles, that show in vitro activity as cytotoxic agents on A2780/S cells and also as cathepsin B inhibitors, synthesis and crystal structure of palladacycles, overview
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additional information
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synthesis and screening of organometallic compounds of general formula [(arene)M(PTA)nXm]Y with metal M = Ru2+, Os2+, Rh3+, or Ir3+, and X = Cl or mPTA, and Y = OTf, PF6, for cytotoxicity and ability to inhibit cathepsin B in vitro, overview. Thermodynamics in solution for metal complexes adducts with N-acetyl-L-cysteine-N'-methylamide, inhibitor binding kinetics, structure-function relationship, overview
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additional information
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no inhibition by human cystatin B
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additional information
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continuous and binary quantitative structure-activity relationship, QSAR, models to classify cathepsin B inhibition activities of small molecules, high throughput screening, detailed overview
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additional information
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inhibition of cathepsin B increases cell viability in the presence of imatinib
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additional information
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not inhibited by oryzacystatin-1 N-terminal deletion, reverse mutant 1 (T30I), reverse mutant 2 (Q97L), and reverse mutant 3 (T30I, Q97L)
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additional information
concanamycin A is an indirect inhibitor by specific inhibiton of VATPase
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additional information
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the inhibition of cathepsin B causes accumulation of 26-kDa pro-TNF-containing vesicles
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additional information
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growth inhibition of B-16 cells by the palladacycle compounds, overview
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additional information
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cathepsin B inhibitory activity of tetraene lactones from the fungus Talaromyces wortmannii, overview
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additional information
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not inhibitory: Z-FY(tert-butyl)-CHN(2)
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additional information
inhibitory potency of a series benzyloxycarbonyl-Phe-X-diazomethylketone, in which Phe promotes binding at S2 while the amino acid X probes S1. The S1 region of cathepsin L also has the ability to accommodate large hydrophobic side chains. In this respect cathepsin L differs from cathepsin B. Thus benzyloxycarbonyl-Phe-Tyr(O-l-butyl)-diazomethylketone, inactivates cathepsin L with higher efficiency compared to cathepsin B
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additional information
no inhibition with pepstatin A at 0.005 and 0.1 mM
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additional information
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no inhibition with pepstatin A at 0.005 and 0.1 mM
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