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3.4.22.1: cathepsin B

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

Word Map on EC 3.4.22.1

Reaction

Hydrolysis of proteins with broad specificity for peptide bonds. Preferentially cleaves -Arg-Arg-/- bonds in small molecule substrates (thus differing from cathepsin L). In addition to being an endopeptidase, shows peptidyl-dipeptidase activity, liberating C-terminal dipeptides =

Synonyms

AC-5, AC-cathB-1, AC-cathB-2, APP secretase, cat B, CatB, CatB1, Cath B, Cath-B, CathB, cathepsin B, cathepsin B proteinase, cathepsin B-like AC-5, cathepsin B-like counter-defence protein, cathepsin B-like cysteine protease, cathepsin B-like cysteine protease 1, cathepsin B-type cysteine protease, cathepsin B1, cathepsin B2, cathepsin B5, cathepsin Ba, cathepsin II, cathepsin-B, CmCatB1, CmCatB2, CP-2, CPB, CpCathB, CPR-4, CsCB1, CsCB2, CsCB3, CsCB4, CTB, CTSB, cysteine cathepsin, DEVDase, LycCatB, MmeCB, More, Na-CP-2, Na-CP-3, Na-CP-4, Na-CP-5, NbCathB, nfcpb, nfcpb-L, PcCTSB, rFgCatB2, Sm31, SmCatB, SmCB1, toxopain-1, TrCB1.1, TrCB1.2, TrCB1.3, TrCB1.4, TrCB1.5, TrCB1.6, TsCPB2

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.1 cathepsin B

Inhibitors

Inhibitors on EC 3.4.22.1 - cathepsin B

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
-
-
1,10-phenanthroline
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
2,2'-dipyridyl disulfide
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-naphthyl-alanine
-
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-DEVD-CHO
-
-
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
AMF4
IC50: 0.00062 mM
ammonium 1-tribromo-1,3,2-dioxatellurolane
-
-
ammonium 1-trichloro-1,3,2-dioxatellurolane
-
-
ankyrin repeat protein
i.e. DARPin 8h6
-
antipain
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
bafilomycin
-
-
bafilomycin A1
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
-
-
BzlNH-tES-Ile-Pro-OH
-
-
CA-030
and derivatives
CA-074
CA-074 Me
Ca-074 methyl ester
CA-074-Me
CA-074-OMe
-
blocks cysteine cathepsins in addition to CatB in in primary human antigen-presenting cells
CA-074Me
CA028
irreversible inhibition, IC50: 0.000140 mM
CA030
CA074
CA074Me
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
canecystatin-1
-
-
-
canecystatin-4
-
-
-
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
-
chicken cystatin
-
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)
-
-
Chloroquine
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)
-
-
chymostatin
CID 11834381
-
-
CID 11834389
-
-
CID 11834392
-
-
CID 1506381
-
-
CID 2212050
-
-
CID 286532
-
-
CID 2998380
-
-
CID 3236798
-
-
CID 3240114
-
-
CID 3241895
-
-
CID 3243025
-
-
CID 3243128
-
-
CID 3243168
-
-
CID 3250046
-
-
CID 3685806
-
-
CID 5293426
-
-
CID 573353
-
-
CID 646525
-
-
CID 646749
-
-
CID 647501
-
-
CID 647599
-
-
CID 648315
-
-
CID 651936
-
-
CID 653297
-
-
CID 653316
-
-
CID 653862
-
-
CID 654815
-
-
CID 655490
-
-
CID 658111
-
-
CID 658152
-
-
CID 658724
-
-
CID 658964
-
-
CID 660829
-
-
CID 66541
-
-
CID 665480
-
-
CID 714967
-
-
CID 794694
-
-
CID 971438
-
-
CLIK148
-
-
CPI-H
-
peptide inhibitor of 13 kDa from rabbit skeletal muscle, noncompetitive
-
CPI-L
-
peptide inhibitor of 23 kDa from rabbit skeletal muscle, noncompetitive
-
Cys (S-benzyl)
-
CysC
-
natural inhibitor of CatB. CysC deletion in knockout mice leads to an enhanced CatB activity
cystatin
-
cystatin C
-
DCG-04
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)
-
-
Dimethylsulfoxide
-
-
doxorubicin
-
-
E-64c
E-64d
EDTA
89% remaining activity at 1 mM, 80% remaining activity at 2 mM
Elastatinal
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-Gly-Pro-OH
-
-
EtO-tES-Ile-Ala-OH
-
-
EtO-tES-Ile-Ile-OH
-
-
EtO-tES-Ile-OH
-
-
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
H2O2
-
-
heparin
-
inhibition is strongly dependent on pH, no inhibition above pH 7.0
HIF
IC50: 0.00058 mM
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
homophenylalanine
-
human albutensin A
-
i.e. AFKAWAVAR
human cystatin A
-
human cystatin B
-
-
-
Human cystatin C
-
iodoacetamide
iodoacetic acid
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
leupeptin
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
myricetin
-
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-ethylmaleimide
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
-
NC-2300
Ni2+
-
26.7% residual activity at 1 mM
NS-196
-
0.0005 mM
oryzacystatin-1
-
-
-
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-chloromercuribenzoate
p-chloromercuriphenyl sulfonic acid
p-hydroxymercuribenzoate
-
-
Pefabloc SC
1.0 mM, 11% loss of activity
penetratin
-
-
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
-
-
Proteinase inhibitors
-
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
-
quercetin
-
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
-
Ser-(O-benzyl)
-
sheep cystatin B
-
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
-
-
Thr (O-tert-butyl)
-
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]
-
-
-
additional information
-