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3.4.22.52: calpain-1

This is an abbreviated version!
For detailed information about calpain-1, go to the full flat file.

Word Map on EC 3.4.22.52

Reaction

broad endopeptidase specificity =

Synonyms

Cal 1, calcium-activated neutral protease I, calpain 1, calpain 1-gamma, calpain 1A, calpain I, calpain small subunit, calpain-1, calpain-1 (micro-form), calpain-I, calpain1, CANP1, CAPN1, CAPN1 g.p. (Homo sapiens), CAPN2, CAPNS1, cysteine protease, EC 3.4.22.17, EC 3.4.24.5, m-CANP, micro-calpain, mit-CPN1, mito-mu-calpain, mu-calpain, muCANP, muI-II

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.52 calpain-1

Inhibitors

Inhibitors on EC 3.4.22.52 - calpain-1

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2,3-di-oxopropyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester
-
SNJ-1945
(-)-epicatechin 5-gallate
-
-
(2R)-N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-6-oxopiperidine-2-carboxamide
-
(2S)-2-[[(4-fluorophenyl)sulfonyl]amino]-N-[(3S)-2-hydroxytetrahydrofuran-3-yl]-3-methylbutanamide
-
-
(2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester
-
broad-spectrum calpain inhibitor
(2S,5S)-5-benzyl-6-hydroxy-2-(2-methylpropyl)morpholin-3-one
-
SNJ-1757
(3S)-2-hydroxytetrahydrofuran-3-yl N-[(10H-phenothiazin-2-yloxy)acetyl]-L-threonyl-L-leucinate
-
-
(3S)-2-hydroxytetrahydrofuran-3-yl N-[(2S)-2-[[(10H-phenothiazin-2-yloxy)acetyl]amino]butanoyl]-L-leucinate
-
-
(3S)-3-[[N-(10H-phenothiazin-2-ylcarbonyl)-L-norvalyl]amino]tetrahydrofuran-2-yl acetate
-
BN-82270
(4R)-N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-benzyl-1-methyl-2-oxoimidazolidine-4-carboxamide
-
(4S)-3-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-1,3-thiazolidine-4-carboxamide
-
-
(4S)-N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-4-methyl-5-oxo-D-prolinamide
-
(6S,9S,16R)-6-(hydroxymethyl)-9-(2-methylpropyl)-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-8,11,14-trione
-
-
(6S,9S,16R)-9-(2-methylpropyl)-8,11,14-trioxo-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-6-carbaldehyde
-
less potent inhibitor with greater than 2fold selectivity for ovine calpain 1 over calpain 2
(7S,10S,13S,26S)-13,26-dibenzyl-7-methyl-10-(propan-2-yl)-5,7,8,10,11,13,14,25,26,28-decahydrotetrabenzo[k,m,t,v][1,4,7,10,15,18]hexaazacyclotetracosine-6,9,12,15,24,27-hexone
-
-
(7S,10S,17R)-10-(2-methylpropyl)-9,12,15-trioxo-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-7-carbaldehyde
-
potent inhibitor of calpain with greater than 7fold selectivity for ovine calpain 2 over ovine calpain 1
(7S,10S,17R)-7-(hydroxymethyl)-10-(2-methylpropyl)-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-9,12,15-trione
-
-
(8S,11S,18R)-11-(2-methylpropyl)-10,13,16-trioxo-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-8-carbaldehyde
-
-
(8S,11S,18R)-8-(hydroxymethyl)-11-(2-methylpropyl)-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-10,13,16-trione
-
-
(9R,12S,19R)-12-(2-methylpropyl)-11,14,17-trioxo-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-9-carbaldehyde
-
-
(9R,12S,19R)-9-(hydroxymethyl)-12-(2-methylpropyl)-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-11,14,17-trione
-
-
([(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]oxy)ethynyl (2Z)-[(3R)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
-
-
1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetra(acetoxymethyl) ester
-
-
1-(2-chloro-4-hydroxyphenyl)-4-oxo-7-(pyridin-4-yl)-1,4-dihydroquinoline-3-carboxamide
-
-
1-(2-chlorobenzyl)-N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
1-benzyl-N-[3,4-dioxo-1-phenyl-4-(phenylamino)butan-2-yl]-5-oxo-D-prolinamide
-
1-benzyl-N-[4-(cyclobutylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
1-benzyl-N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
1-benzyl-N-[4-(ethylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
1-benzyl-N-[4-(methoxyamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
1-benzyl-N-[4-[(4-fluorophenyl)amino]-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
1-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-D-prolinamide
-
-
2-methyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-7,8-dihydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
-
3,4-dichlorophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 56 nM
3,4-dichlorophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 56 nM
3-([4-[2-(methoxymethoxy)phenyl]-4-oxobutanoyl]amino)-2-oxo-4-phenylbutanamide
-
reversible inhibitor
3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoic acid
-
reversible inhibitor
3-acetyl-2-[(2,4-dichlorophenyl)amino]-8-(trifluoromethyl)quinolin-4(1H)-one
-
-
3-acetyl-2-[(3-fluorophenyl)amino]-8-phenylquinolin-4(1H)-one
-
-
3-acetyl-2-[(4-chlorophenyl)amino]-5,8-difluoroquinolin-4(1H)-one
-
-
3-acetyl-2-[(4-tert-butylphenyl)amino]-5,8-difluoroquinolin-4(1H)-one
-
-
3-acetyl-2-[(4-tert-butylphenyl)amino]-8-chloro-6-nitroquinolin-4(1H)-one
-
-
3-acetyl-2-[[3,5-bis(trifluoromethyl)phenyl]amino]-5,8-difluoroquinolin-4(1H)-one
-
-
3-acetyl-5,8-dibromo-2-[(4-bromophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-5,8-dichloro-2-[(2,4-dichlorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-6,8-difluoro-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-6-chloro-2-[(2,4-dichlorophenyl)amino]-8-nitroquinolin-4(1H)-one
-
-
3-acetyl-6-chloro-2-[(2-chloro-4-methylphenyl)amino]-8-nitroquinolin-4(1H)-one
-
-
3-acetyl-6-chloro-8-(trifluoromethyl)-2-[[4-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one
-
-
3-acetyl-7,8-dichloro-2-[[3-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one
-
-
3-acetyl-8-bromo-5-chloro-2-[(4-chlorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(2,4-dibromophenyl)amino]-5-methylquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(2-fluoro-5-methylphenyl)amino]-5-(trifluoromethyl)quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(3-methylphenyl)amino]-5-nitroquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(4-chloro-2-fluorophenyl)amino]-5-methylquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(4-chlorophenyl)amino]-6-nitroquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-5-fluoro-2-(phenylamino)quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-5-methyl-2-[(2,3,4-trifluorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-5-methyl-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one
-
-
4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoic acid
-
reversible inhibitor
4-fluorophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 29 nM
4-fluorophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 50 nM
4-nitrophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 47 nM
4-nitrophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 50 nM
4-[([(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]oxy)methyl]benzyl (2Z)-[(3R)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
-
-
5-azanylidyne-N-[[(2S,3S)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-norvalyl-L-arginyl-L-tryptophanamide
-
irreversible inhibitor
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-1H-pyrrole-2-carboxamide
-
CAT0059
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]furan-2-carboxamide
-
-
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]thiophene-2-carboxamide
-
-
A23187
-
-
acetyl-calpastatin peptide
-
50 microM
-
acetyl-DPMSSTYIEE-betaAla-GKREVTIPPKYRELLA-NH2
-
-
acetyl-DPMSSTYIEELGK-NH2
-
-
acetyl-DPMSSTYIEELGKREVT-betaAla-PPKYRELLA-NH2
-
-
acetyl-DPMSSTYIEELGKREVTIPPKYR-NH2
-
-
acetyl-DPMSSTYIEELGKREVTIPPKYREL-NH2
-
-
acetyl-DPMSSTYIEELGKREVTIPPKYRELLA-NH2
-
CP1B peptide
acetyl-Leu-Leu-Met-CHO
-
-
acetyl-Leu-Leu-Nle-CHO
acetyl-REVTIPPKYRELLA-NH2
-
-
acetyl-RRMKWKKDPMSSTYIEELGKREVTIPPKYRELLA-NH2
-
-
acetyl-RYKPPITVERKGLEEIYTSS-NH2
-
-
acetyl-SSTTYIEELGKREVTIPPKYR-NH2
-
-
acetyl-SSTYIEELGK-NH-(CH2O)2-CH2C(O)-TIPPKYR-NH2
-
-
acetyl-SSTYIEELGKREVTIPPK-NH2
-
-
acetyl-SSTYIEELGKREVTIPPKYR-NH2
-
-
acetyl-SSTYIEELGKREVTIPPKYRELLA-NH2
-
-
acetyl-TYIEELGKREVTIPPKYR-NH2
-
-
acetyl-TYIEELGKREVTIPPKYRELLA-NH2
-
-
AK-275
-
reversible inhibitor
-
AK-295
AK-295-D1
-
reversible inhibitor
-
AK-295-D2
-
reversible inhibitor
-
Al3+
-
inactivates enzyme from smooth muscle at millimolar concentrations of Ca2+, calpain 1 and 2
ALLM
-
reversible inhibitor
antipain
-
0.01 mM, 80-90% inhibition
benzyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate
-
-
benzyl [(6S,9S,12S)-6-formyl-9-(2-methylpropyl)-8,11-dioxo-2-oxa-7,10-diazabicyclo[12.2.2]octadeca-1(16),14,17-trien-12-yl]carbamate
-
-
benzyl [(7S,10S,13S)-7-formyl-10-(2-methylpropyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-trien-13-yl]carbamate
-
CAT811
benzyl [(8S,11S,14S)-8-formyl-11-(2-methylpropyl)-10,13-dioxo-2-oxa-9,12-diazabicyclo[14.2.2]icosa-1(18),16,19-trien-14-yl]carbamate
-
-
butyl (2Z)-[(3S)-3-(butan-2-yl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
-
-
Calmidazolium
-
-
calpain inhibitor 1
-
synthetic calpain inhibitor
calpain inhibitor III
calpain inhibitor peptide III
-
-
calpain inhibitor VI
-
-
calpain inhibitor-1
calpain inhibitor-III
calpain VI inhibitor
-
calpastatin
-
calpastatin 1
-
calpain 1 is under constant inhibiting effect of active calpastatin 1
-
calpastatin peptides
-
-
-
calpeptin
carbobenzoxy-valinyl-phenylalaninal
-
-
CP1B peptide
-
a 20-mer peptide truncated from region B of calpastatin inhibitory domain 1, 1000fold more selective for mu-calpain than cathepsin L
-
cystatin
-
engineered cystatins. Recombinant hybrids of human stefin B with KS2 and DELTAL110 deletion mutants of chicken cystatin-KD2 hybrids. Substitution of the N-terminal contact region of stefin B by ther corresponding KD2 sequence results in a calpain inhibitor with a Ki-value of 188 nM. Deletion of L110 improves inhibition 4 to 8fold. All engineered cystatins are temporary inhibitors
-
dimethyl (2S,2'S)-2,2'-[biphenyl-2,2'-diylbis(carbonylimino)]bis(3-phenylpropanoate)
-
-
DPMSSTYIEELGKREVTIPPKYRELLA
-
2 hot spots are detected in which the residues critical for inhibitory function are clustered: Leu11-Gly12 and Thr17-Ile18-Pro19
E-64c
E-64d
-
irreversible inhibitor
E64d
-
-
EGTA
-
-
Ep-460
-
irreversible inhibitor
ethyl 3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoate
-
reversible inhibitor
ethyl 4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoate
-
reversible inhibitor
heat shock protein 90
-
incubation of calpain-1 at a molar ratio of 1:1 with heat shock protein 90, at increasing Ca2+ concentrations, results in a significant decrease of calpain proteolytic activity at [Ca2+] up to 0.04 mM. At higher Ca2+ concentrations, the inhibiting effect of heat shock protein 90 is no more detectable
-
inhibitor protein Ci1
-
non-specific inhibitor
-
iodoacetic acid
-
0.25 mM, complete
ionomycin
-
-
lactacystin
-
1 microM
leupeptin
MDL-28170
MDL-28710
-
complete inhibition at 100 nM
MDL28170
methyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 89 nM
methyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate
-
-
methyl (3S)-4-cyclohexyl-3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxobutanoate
-
IC50: 1000 nM
methyl (S,S,Z)-(3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-ylidene)acetate
-
strong inhibitor
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucinate
-
-
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucyl-L-isoleucinate
-
-
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-leucyl-L-phenylalaninate
-
-
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-valyl-L-phenylalaninate
-
-
methyl N-[[2'-([(2S)-1-[(2'-aminobiphenyl-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl)biphenyl-2-yl]carbonyl]-L-phenylalanyl-L-valinate
-
-
MG115
-
inhibitory effect in micromolar concentrations, 1 mircoM
MG132
N'-((1S,2R)-1-benzyl-3-[(3,5-dimethoxybenzyl)amino]-2-hydroxypropyl)-N,N-dipropylbenzene-1,3-dicarboxamide
-
IC50: 20 nM
N-((1S)-1-benzyl-2,3-dioxo-3-[(2-phenylethyl)amino]propyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 63 nM
N-((1S)-1-benzyl-3-[(1-methylethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 205 nM
N-((1S)-1-benzyl-3-[(2-methoxyethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 200 nM
N-((1S)-1-benzyl-3-[(cyclopropylmethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 286 nM
N-((1S)-1-[(butylamino)(oxo)acetyl]-3-methylbutyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
-
N-(1-amino-1,2-dioxoheptan-3-yl)-1-benzyl-5-oxo-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(1-benzothiophen-2-ylcarbonyl)piperidine-4-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(2,2-dimethylpropyl)-5-oxo-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(cyclohexylmethyl)-5-oxo-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-5-oxo-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-5-oxo-L-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-6-oxo-1,6-dihydropyridine-2-carboxamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-[(4-methylphenyl)sulfonyl]-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-[2-methoxy-6-(trifluoromethyl)benzyl]-5-oxo-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-2-benzyl-1,2-thiazolidine-3-carboxamide 1,1-dioxide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-2-[(E)-2-[4-[(diethylamino)methyl]phenyl]ethenyl]benzamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-1,4-dihydroquinoline-2-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-4H-chromene-2-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-4-methyl-6-methylidene-1,6-dihydropyridine-3-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-(pyridin-4-ylmethyl)-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[2-(trifluoromethoxy)benzyl]-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[2-(trifluoromethyl)benzyl]-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[3-(trifluoromethoxy)benzyl]-D-prolinamide
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[3-(trifluoromethyl)benzyl]-D-prolinamide
-
N-acetyl-L-Leu-L-Leu-L-Met
-
-
N-acetyl-L-leucyl-L-leucyl-L-norleucinal
-
broad-spectrum calpain inhibitor
N-acetyl-Leu-Leu-Nle-CHO
-
complete inhibition at 0.5 mM
N-acetyl-Leu-Leu-Norleu-al
-
-
N-acetyl-Leu-Leu-norleucinal
-
2-fold increase in Tat levels after pre-treating with ALLN, 10 microM
N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-tyrosyl fluoromethylketone
-
broad-spectrum calpain inhibitor
N-[(1S)-1-benzyl-2,3-dioxo-3-(pentylamino)propyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 150 nM
N-[(1S)-1-benzyl-2,3-dioxo-3-(prop-2-en-1-ylamino)propyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 200 nM
N-[(1S)-1-benzyl-2-oxoethyl]-N2-[(benzyloxy)carbonyl]-L-leucinamide
-
-
N-[(1S)-1-benzyl-3-(benzylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 81 nM
N-[(1S)-1-benzyl-3-(butylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
-
N-[(1S)-1-benzyl-3-(ethylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 340 nM
N-[(2S)-1-oxo-3-phenylpropan-2-yl]-7,8-dihydro-2H-[1,4]dioxino[2,3-g][1,2,4]benzothiadiazine-3-carboxamide 1,1-dioxide
-
-
N-[(2S)-1-[[(3S)-2-hydroxytetrahydrofuran-3-yl]amino]-1-oxopentan-2-yl]-10H-phenothiazine-2-carboxamide
-
BN-82204
N-[(2S)-3,4-dioxo-1-phenyl-4-([3-[(phenylsulfonyl)amino]propyl]amino)butan-2-yl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
reversible inhibitor
N-[(2S)-4-(2-benzylhydrazinyl)-3,4-dioxo-1-phenylbutan-2-yl]-N2-[(benzyloxy)carbonyl]-L-leucinamide
-
reversible inhibitor
N-[(2S)-4-(butylamino)-3,4-dioxo-1-phenylbutan-2-yl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
reversible inhibitor
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-fluoro-1-(4-hydroxyphenyl)-3-oxobutan-2-yl]-L-leucinamide
-
irreversible inhibitor
N-[1-(4-bromophenyl)-4-(ethylamino)-3,4-dioxobutan-2-yl]-N2-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucinamide
-
reversible inhibitor
N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-1-(1-methyl-1H-pyrazol-4-yl)-5-oxo-D-prolinamide
-
N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-1-(2,3-dihydro-1H-inden-2-yl)-5-oxo-D-prolinamide
-
N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-1-[2-(trifluoromethoxy)-6-(trifluoromethyl)benzyl]-D-prolinamide
-
N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-1-[2-(trifluoromethoxy)benzyl]-D-prolinamide
-
N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-1-[2-(trifluoromethyl)benzyl]-D-prolinamide
-
N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide
-
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide
-
-
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-oxopentan-2-yl]-L-leucinamide
-
potent inhibitor with more than 2.5fold selectivity for ovine calpain 1 over ovine calpain 2
N-[[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-histidyl-L-arginyl-L-tryptophanamide
-
irreversible inhibitor
N2-[(2S)-2-([[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]amino)pent-4-enoyl]-L-arginyl-L-tryptophanamide
-
irreversible inhibitor
N2-[(benzyloxy)carbonyl]-N-[4-(ethylamino)-3,4-dioxo-1-phenylbutan-2-yl]-L-leucinamide
-
reversible inhibitor
NaCl
-
mu-calpain is more active at 165 mM NaCl than at 295 mM NaCl
PCP1B peptide
-
-
-
PD-150606
-
-
PD-151746
-
-
PD150606
penetratin
-
-
penicillide
-
-
pepstatin A
-
1 mM, 60-80% inhibition
phenyl (2-[(3-([(1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 76 nM
phenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 40 nM
phenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 35 nM
ritonavir
-
also inhibits calcium-stimulated calpain activity in PC12 cells in situ. Ritonavir or analogues of the drug should by investigated as cytoprotective agents in conditions where cell death or injury is mediated via calpain activation
SJA-6017
-
reversible inhibitor
SNJ-1715
-
reversible inhibitor
SNJ-1945
SNJ1715
-
-
TLCK
-
0.1 mM, 60-80% inhibition
Z-Val-Phe-CHO
-
i.e. MDL-28710, 1.0 microM
ZLLY-CH2F
-
irreversible inhibitor
additional information
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