3.4.22.52 ((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2,3-di-oxopropyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester SNJ-1945 160147 3.4.22.52 (-)-epicatechin 5-gallate - 160138 3.4.22.52 (2R)-N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-6-oxopiperidine-2-carboxamide - 235440 3.4.22.52 (2S)-2-[[(4-fluorophenyl)sulfonyl]amino]-N-[(3S)-2-hydroxytetrahydrofuran-3-yl]-3-methylbutanamide - 81246 3.4.22.52 (2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester broad-spectrum calpain inhibitor 33021 3.4.22.52 (2S,5S)-5-benzyl-6-hydroxy-2-(2-methylpropyl)morpholin-3-one SNJ-1757 81247 3.4.22.52 (3S)-2-hydroxytetrahydrofuran-3-yl N-[(10H-phenothiazin-2-yloxy)acetyl]-L-threonyl-L-leucinate - 81251 3.4.22.52 (3S)-2-hydroxytetrahydrofuran-3-yl N-[(2S)-2-[[(10H-phenothiazin-2-yloxy)acetyl]amino]butanoyl]-L-leucinate - 81250 3.4.22.52 (3S)-3-[[N-(10H-phenothiazin-2-ylcarbonyl)-L-norvalyl]amino]tetrahydrofuran-2-yl acetate BN-82270 81249 3.4.22.52 (4R)-N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-benzyl-1-methyl-2-oxoimidazolidine-4-carboxamide - 235617 3.4.22.52 (4S)-3-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-1,3-thiazolidine-4-carboxamide - 160139 3.4.22.52 (4S)-N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-4-methyl-5-oxo-D-prolinamide - 235625 3.4.22.52 (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 - 81297 3.4.22.52 (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 81292 3.4.22.52 (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 - 81270 3.4.22.52 (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 81293 3.4.22.52 (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 - 81298 3.4.22.52 (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 - 81294 3.4.22.52 (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 - 81299 3.4.22.52 (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 - 81295 3.4.22.52 (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 - 81300 3.4.22.52 ([(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 - 65027 3.4.22.52 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetra(acetoxymethyl) ester - 81291 3.4.22.52 1-(2-chloro-4-hydroxyphenyl)-4-oxo-7-(pyridin-4-yl)-1,4-dihydroquinoline-3-carboxamide - 81267 3.4.22.52 1-(2-chlorobenzyl)-N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 235794 3.4.22.52 1-benzyl-N-[3,4-dioxo-1-phenyl-4-(phenylamino)butan-2-yl]-5-oxo-D-prolinamide - 235822 3.4.22.52 1-benzyl-N-[4-(cyclobutylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 235823 3.4.22.52 1-benzyl-N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 235824 3.4.22.52 1-benzyl-N-[4-(ethylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 235825 3.4.22.52 1-benzyl-N-[4-(methoxyamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 235826 3.4.22.52 1-benzyl-N-[4-[(4-fluorophenyl)amino]-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 235827 3.4.22.52 1-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-D-prolinamide - 81237 3.4.22.52 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 - 81238 3.4.22.52 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 58610 3.4.22.52 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 58611 3.4.22.52 3-([4-[2-(methoxymethoxy)phenyl]-4-oxobutanoyl]amino)-2-oxo-4-phenylbutanamide reversible inhibitor 81261 3.4.22.52 3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoic acid reversible inhibitor 81253 3.4.22.52 3-acetyl-2-[(2,4-dichlorophenyl)amino]-8-(trifluoromethyl)quinolin-4(1H)-one - 81276 3.4.22.52 3-acetyl-2-[(3-fluorophenyl)amino]-8-phenylquinolin-4(1H)-one - 81277 3.4.22.52 3-acetyl-2-[(4-chlorophenyl)amino]-5,8-difluoroquinolin-4(1H)-one - 81281 3.4.22.52 3-acetyl-2-[(4-tert-butylphenyl)amino]-5,8-difluoroquinolin-4(1H)-one - 81280 3.4.22.52 3-acetyl-2-[(4-tert-butylphenyl)amino]-8-chloro-6-nitroquinolin-4(1H)-one - 40420 3.4.22.52 3-acetyl-2-[[3,5-bis(trifluoromethyl)phenyl]amino]-5,8-difluoroquinolin-4(1H)-one - 81282 3.4.22.52 3-acetyl-5,8-dibromo-2-[(4-bromophenyl)amino]quinolin-4(1H)-one - 40423 3.4.22.52 3-acetyl-5,8-dichloro-2-[(2,4-dichlorophenyl)amino]quinolin-4(1H)-one - 40425 3.4.22.52 3-acetyl-6,8-difluoro-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one - 81287 3.4.22.52 3-acetyl-6-chloro-2-[(2,4-dichlorophenyl)amino]-8-nitroquinolin-4(1H)-one - 40422 3.4.22.52 3-acetyl-6-chloro-2-[(2-chloro-4-methylphenyl)amino]-8-nitroquinolin-4(1H)-one - 40421 3.4.22.52 3-acetyl-6-chloro-8-(trifluoromethyl)-2-[[4-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one - 81275 3.4.22.52 3-acetyl-7,8-dichloro-2-[[3-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one - 81274 3.4.22.52 3-acetyl-8-bromo-5-chloro-2-[(4-chlorophenyl)amino]quinolin-4(1H)-one - 40424 3.4.22.52 3-acetyl-8-chloro-2-[(2,4-dibromophenyl)amino]-5-methylquinolin-4(1H)-one - 19234 3.4.22.52 3-acetyl-8-chloro-2-[(2-fluoro-5-methylphenyl)amino]-5-(trifluoromethyl)quinolin-4(1H)-one - 81286 3.4.22.52 3-acetyl-8-chloro-2-[(3-methylphenyl)amino]-5-nitroquinolin-4(1H)-one - 81278 3.4.22.52 3-acetyl-8-chloro-2-[(4-chloro-2-fluorophenyl)amino]-5-methylquinolin-4(1H)-one - 81283 3.4.22.52 3-acetyl-8-chloro-2-[(4-chlorophenyl)amino]-6-nitroquinolin-4(1H)-one - 40419 3.4.22.52 3-acetyl-8-chloro-5-fluoro-2-(phenylamino)quinolin-4(1H)-one - 81279 3.4.22.52 3-acetyl-8-chloro-5-methyl-2-[(2,3,4-trifluorophenyl)amino]quinolin-4(1H)-one - 81285 3.4.22.52 3-acetyl-8-chloro-5-methyl-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one - 81284 3.4.22.52 4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoic acid reversible inhibitor 81256 3.4.22.52 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 58612 3.4.22.52 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 58613 3.4.22.52 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 58608 3.4.22.52 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 58609 3.4.22.52 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 - 65510 3.4.22.52 5-azanylidyne-N-[[(2S,3S)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-norvalyl-L-arginyl-L-tryptophanamide irreversible inhibitor 81272 3.4.22.52 5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-1H-pyrrole-2-carboxamide CAT0059 81240 3.4.22.52 5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]furan-2-carboxamide - 81241 3.4.22.52 5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]thiophene-2-carboxamide - 81242 3.4.22.52 A23187 - 3321 3.4.22.52 acetyl-calpastatin peptide 50 microM 151751 3.4.22.52 acetyl-DPMSSTYIEE-betaAla-GKREVTIPPKYRELLA-NH2 - 81231 3.4.22.52 acetyl-DPMSSTYIEELGK-NH2 - 66563 3.4.22.52 acetyl-DPMSSTYIEELGKREVT-betaAla-PPKYRELLA-NH2 - 81232 3.4.22.52 acetyl-DPMSSTYIEELGKREVTIPPKYR-NH2 - 66560 3.4.22.52 acetyl-DPMSSTYIEELGKREVTIPPKYREL-NH2 - 66559 3.4.22.52 acetyl-DPMSSTYIEELGKREVTIPPKYRELLA-NH2 CP1B peptide 81230 3.4.22.52 acetyl-Leu-Leu-Met-CHO - 81290 3.4.22.52 acetyl-Leu-Leu-Nle-CHO - 10273 3.4.22.52 acetyl-Leu-Leu-Nle-CHO a calpain inhibitor 10273 3.4.22.52 acetyl-REVTIPPKYRELLA-NH2 - 66564 3.4.22.52 acetyl-RRMKWKKDPMSSTYIEELGKREVTIPPKYRELLA-NH2 - 81234 3.4.22.52 acetyl-RYKPPITVERKGLEEIYTSS-NH2 - 66566 3.4.22.52 acetyl-SSTTYIEELGKREVTIPPKYR-NH2 - 81235 3.4.22.52 acetyl-SSTYIEELGK-NH-(CH2O)2-CH2C(O)-TIPPKYR-NH2 - 66565 3.4.22.52 acetyl-SSTYIEELGKREVTIPPK-NH2 - 66562 3.4.22.52 acetyl-SSTYIEELGKREVTIPPKYR-NH2 - 66561 3.4.22.52 acetyl-SSTYIEELGKREVTIPPKYRELLA-NH2 - 66557 3.4.22.52 acetyl-TYIEELGKREVTIPPKYR-NH2 - 25056 3.4.22.52 acetyl-TYIEELGKREVTIPPKYRELLA-NH2 - 66558 3.4.22.52 AK-275 reversible inhibitor 160134 3.4.22.52 AK-295 reversible inhibitor 81236 3.4.22.52 AK-295 - 81236 3.4.22.52 AK-295-D1 reversible inhibitor 160130 3.4.22.52 AK-295-D2 reversible inhibitor 160131 3.4.22.52 Al3+ inactivates enzyme from smooth muscle at millimolar concentrations of Ca2+, calpain 1 and 2 264 3.4.22.52 ALLM reversible inhibitor 40418 3.4.22.52 ALLN reversible inhibitor 25515 3.4.22.52 ALLN - 25515 3.4.22.52 antipain 0.01 mM, 80-90% inhibition 520 3.4.22.52 benzyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate - 65700 3.4.22.52 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 - 81243 3.4.22.52 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 81244 3.4.22.52 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 - 81245 3.4.22.52 butyl (2Z)-[(3S)-3-(butan-2-yl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate - 160146 3.4.22.52 Calmidazolium - 3621 3.4.22.52 calpain inhibitor 1 synthetic calpain inhibitor 160145 3.4.22.52 calpain inhibitor III - 27585 3.4.22.52 calpain inhibitor peptide III - 160148 3.4.22.52 calpain inhibitor VI - 81288 3.4.22.52 calpain inhibitor-1 - 66556 3.4.22.52 calpain inhibitor-III - 81229 3.4.22.52 calpain inhibitor-III completely inhibited by 0.01 mM 81229 3.4.22.52 calpain VI inhibitor 78 nM used in assay conditions 201836 3.4.22.52 calpastatin - 1386 3.4.22.52 calpastatin inhibition of mu-calpain is higher at 295 mM NaCl than at 165 mM. Inhibition is not altered by pH from pH 6.0-7.5 1386 3.4.22.52 calpastatin oxidation lowers calpastatin inhibition of mu-calpain at al pH and ionic strength combinations 1386 3.4.22.52 calpastatin mitochondrial mu-calpain is tightly regulated by its endogenous inhibitor calpastatin 1386 3.4.22.52 calpastatin highly specific inhibitor of calpain-1 and calpain-2 1386 3.4.22.52 calpastatin broad-spectrum calpain inhibitor 1386 3.4.22.52 calpastatin highly specific calpain inhibitor 1386 3.4.22.52 calpastatin the occurrence of a complex between heat shock protein 90 and calpain-1, in which the protease is still activable, can prevent the complete inhibition of the protease even in the presence of high calpastatin levels 1386 3.4.22.52 calpastatin 1 calpain 1 is under constant inhibiting effect of active calpastatin 1 113168 3.4.22.52 calpastatin peptides - 139106 3.4.22.52 calpeptin - 2399 3.4.22.52 calpeptin reversible inhibitor 2399 3.4.22.52 calpeptin Z-Leu-Nle-CHO 2399 3.4.22.52 calpeptin complete inhibition at 0.5 mM 2399 3.4.22.52 carbobenzoxy-valinyl-phenylalaninal - 81273 3.4.22.52 CP1B peptide a 20-mer peptide truncated from region B of calpastatin inhibitory domain 1, 1000fold more selective for mu-calpain than cathepsin L 81228 3.4.22.52 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 1600 3.4.22.52 dimethyl (2S,2'S)-2,2'-[biphenyl-2,2'-diylbis(carbonylimino)]bis(3-phenylpropanoate) - 81268 3.4.22.52 DPMSSTYIEELGKREVTIPPKYRELLA 2 hot spots are detected in which the residues critical for inhibitory function are clustered: Leu11-Gly12 and Thr17-Ile18-Pro19 113350 3.4.22.52 E-64 0.05 mg/ml, complete inhibition 559 3.4.22.52 E-64 - 559 3.4.22.52 E-64 irreversible inhibitor 559 3.4.22.52 E-64c 0.01 mM, 80-90% inhibition 13400 3.4.22.52 E-64c irreversible inhibitor 13400 3.4.22.52 E-64d irreversible inhibitor 7673 3.4.22.52 E64 - 1457 3.4.22.52 E64d - 18966 3.4.22.52 EDTA 0.25 mM, complete 21 3.4.22.52 EDTA - 21 3.4.22.52 EGTA - 173 3.4.22.52 Ep-460 irreversible inhibitor 31449 3.4.22.52 ethyl 3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoate reversible inhibitor 81252 3.4.22.52 ethyl 4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoate reversible inhibitor 81255 3.4.22.52 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 40727 3.4.22.52 inhibitor protein Ci1 non-specific inhibitor 151750 3.4.22.52 iodoacetic acid 0.25 mM, complete 213 3.4.22.52 ionomycin - 4394 3.4.22.52 lactacystin 1 microM 2107 3.4.22.52 leupeptin 0.05 mg/ml, complete inhibition 217 3.4.22.52 leupeptin - 217 3.4.22.52 leupeptin 0.01 mM, 80-90% inhibition 217 3.4.22.52 leupeptin a naturally occurring calpain inhibitor 217 3.4.22.52 leupeptin reversible inhibitor 217 3.4.22.52 MDL-28170 reversible inhibitor 11631 3.4.22.52 MDL-28170 Cbz-Val-Phel-alanial 11631 3.4.22.52 MDL-28170 - 11631 3.4.22.52 MDL-28710 complete inhibition at 100 nM 136451 3.4.22.52 MDL28170 - 8857 3.4.22.52 MDL28170 potent inhibitor of the active site of calpain1 8857 3.4.22.52 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 58604 3.4.22.52 methyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate - 65737 3.4.22.52 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 58595 3.4.22.52 methyl (S,S,Z)-(3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-ylidene)acetate strong inhibitor 81289 3.4.22.52 methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucinate - 65785 3.4.22.52 methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucyl-L-isoleucinate - 65786 3.4.22.52 methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-leucyl-L-phenylalaninate - 65787 3.4.22.52 methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-valyl-L-phenylalaninate - 65788 3.4.22.52 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 - 81269 3.4.22.52 MG115 inhibitory effect in micromolar concentrations, 1 mircoM 33829 3.4.22.52 MG132 inhibitory effect in micromolar concentrations, 1 microM 2689 3.4.22.52 MG132 - 2689 3.4.22.52 additional information specific capn1 shRNA reduces expression of the targeted isoform 2 3.4.22.52 additional information FANCA and FANCG proteins bind directly to mu-calpain, this binding may lead to inhibition of mu-calpain activity in normal cells 2 3.4.22.52 N'-((1S,2R)-1-benzyl-3-[(3,5-dimethoxybenzyl)amino]-2-hydroxypropyl)-N,N-dipropylbenzene-1,3-dicarboxamide IC50: 20 nM 58614 3.4.22.52 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 58602 3.4.22.52 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 58598 3.4.22.52 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 58597 3.4.22.52 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 58599 3.4.22.52 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 - 129500 3.4.22.52 N-(1-amino-1,2-dioxoheptan-3-yl)-1-benzyl-5-oxo-D-prolinamide - 236560 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(1-benzothiophen-2-ylcarbonyl)piperidine-4-carboxamide reversible inhibitor 81265 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(2,2-dimethylpropyl)-5-oxo-D-prolinamide - 236636 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(cyclohexylmethyl)-5-oxo-D-prolinamide - 236637 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-5-oxo-D-prolinamide - 236638 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-5-oxo-L-prolinamide - 236639 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-benzyl-6-oxo-1,6-dihydropyridine-2-carboxamide - 236640 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-[(4-methylphenyl)sulfonyl]-D-prolinamide - 236641 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-[2-methoxy-6-(trifluoromethyl)benzyl]-5-oxo-D-prolinamide - 236642 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-2-benzyl-1,2-thiazolidine-3-carboxamide 1,1-dioxide - 236643 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-2-[(E)-2-[4-[(diethylamino)methyl]phenyl]ethenyl]benzamide reversible inhibitor 81266 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-1,4-dihydroquinoline-2-carboxamide reversible inhibitor 81263 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-4H-chromene-2-carboxamide reversible inhibitor 81264 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-4-methyl-6-methylidene-1,6-dihydropyridine-3-carboxamide reversible inhibitor 81262 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-(pyridin-4-ylmethyl)-D-prolinamide - 236644 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[2-(trifluoromethoxy)benzyl]-D-prolinamide - 236645 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[2-(trifluoromethyl)benzyl]-D-prolinamide - 236646 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[3-(trifluoromethoxy)benzyl]-D-prolinamide - 236647 3.4.22.52 N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-5-oxo-1-[3-(trifluoromethyl)benzyl]-D-prolinamide - 236648 3.4.22.52 N-acetyl-L-Leu-L-Leu-L-Met - 160128 3.4.22.52 N-acetyl-L-leucyl-L-leucyl-L-norleucinal broad-spectrum calpain inhibitor 160142 3.4.22.52 N-acetyl-Leu-Leu-Nle-CHO complete inhibition at 0.5 mM 167878 3.4.22.52 N-acetyl-Leu-Leu-Norleu-al - 160144 3.4.22.52 N-acetyl-Leu-Leu-norleucinal 2-fold increase in Tat levels after pre-treating with ALLN, 10 microM 21177 3.4.22.52 N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-tyrosyl fluoromethylketone broad-spectrum calpain inhibitor 160143 3.4.22.52 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 58600 3.4.22.52 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 58603 3.4.22.52 N-[(1S)-1-benzyl-2-oxoethyl]-N2-[(benzyloxy)carbonyl]-L-leucinamide - 65826 3.4.22.52 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 58601 3.4.22.52 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 - 129501 3.4.22.52 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 58596 3.4.22.52 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 - 81239 3.4.22.52 N-[(2S)-1-[[(3S)-2-hydroxytetrahydrofuran-3-yl]amino]-1-oxopentan-2-yl]-10H-phenothiazine-2-carboxamide BN-82204 81248 3.4.22.52 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 81260 3.4.22.52 N-[(2S)-4-(2-benzylhydrazinyl)-3,4-dioxo-1-phenylbutan-2-yl]-N2-[(benzyloxy)carbonyl]-L-leucinamide reversible inhibitor 81258 3.4.22.52 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 81259 3.4.22.52 N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-fluoro-1-(4-hydroxyphenyl)-3-oxobutan-2-yl]-L-leucinamide irreversible inhibitor 160141 3.4.22.52 N-[1-(4-bromophenyl)-4-(ethylamino)-3,4-dioxobutan-2-yl]-N2-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucinamide reversible inhibitor 81257 3.4.22.52 N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-1-(1-methyl-1H-pyrazol-4-yl)-5-oxo-D-prolinamide - 236914 3.4.22.52 N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-1-(2,3-dihydro-1H-inden-2-yl)-5-oxo-D-prolinamide - 236915 3.4.22.52 N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-1-[2-(trifluoromethoxy)-6-(trifluoromethyl)benzyl]-D-prolinamide - 236916 3.4.22.52 N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-1-[2-(trifluoromethoxy)benzyl]-D-prolinamide - 236917 3.4.22.52 N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-1-[2-(trifluoromethyl)benzyl]-D-prolinamide - 236918 3.4.22.52 N-[4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl]-5-oxo-D-prolinamide - 236919 3.4.22.52 N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide - 81301 3.4.22.52 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 81296 3.4.22.52 N-[[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-histidyl-L-arginyl-L-tryptophanamide irreversible inhibitor 160140 3.4.22.52 N2-[(2S)-2-([[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]amino)pent-4-enoyl]-L-arginyl-L-tryptophanamide irreversible inhibitor 81271 3.4.22.52 N2-[(benzyloxy)carbonyl]-N-[4-(ethylamino)-3,4-dioxo-1-phenylbutan-2-yl]-L-leucinamide reversible inhibitor 81254 3.4.22.52 NaCl mu-calpain is more active at 165 mM NaCl than at 295 mM NaCl 42 3.4.22.52 Pb2+ - 139 3.4.22.52 PCP1B peptide - 81233 3.4.22.52 PD-150606 - 160135 3.4.22.52 PD-151746 - 160136 3.4.22.52 PD150606 - 7903 3.4.22.52 PD150606 specific inhibitor of calpain I 7903 3.4.22.52 penetratin - 22572 3.4.22.52 penicillide - 160137 3.4.22.52 pepstatin A 1 mM, 60-80% inhibition 309 3.4.22.52 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 58605 3.4.22.52 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 58606 3.4.22.52 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 58607 3.4.22.52 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 996 3.4.22.52 SJA-6017 reversible inhibitor 160133 3.4.22.52 SNJ-1715 reversible inhibitor 160129 3.4.22.52 SNJ-1945 reversible inhibitor 40417 3.4.22.52 SNJ-1945 - 40417 3.4.22.52 SNJ1715 - 160149 3.4.22.52 TLCK 0.1 mM, 60-80% inhibition 4621 3.4.22.52 Z-Val-Phe-CHO i.e. MDL-28710, 1.0 microM 63135 3.4.22.52 ZLLY-CH2F irreversible inhibitor 160132