3.4.22.53 (2S)-3-phenyl-2-([[(2S)-1-(phenylsulfonyl)pyrrolidin-2-yl]carbonyl]amino)propanoic acid - 81305 3.4.22.53 (2S)-4-methyl-2-[(phenylsulfonyl)amino]pentanoic acid - 81303 3.4.22.53 (2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester 0.01 mM, 50% inhibition 33021 3.4.22.53 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetra(acetoxymethyl) ester - 81291 3.4.22.53 110 kDa calpastatin - 81306 3.4.22.53 3,4-dichloroisocoumarin 0.05 mM, 11% inhibition 1040 3.4.22.53 4-[[(3,4-dinitrophenyl)carbonyl]amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid 5 mM, 23% inhibition 142923 3.4.22.53 70 kDa calpastatin - 81307 3.4.22.53 Ac-Thr-Pro-Leu-alpha-azaglycine-Ser-Pro-Pro-NH2 - 201840 3.4.22.53 Ac-Thr-Pro-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2 - 201839 3.4.22.53 Ac-Thr-Pro-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-Pro-Arg-NH2 - 201838 3.4.22.53 Ac-Thr-Ser-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2 - 201842 3.4.22.53 Ac-Thr-Trp-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2 - 201841 3.4.22.53 acetyl-Leu-Leu-Met-CHO selectively inhibits the activity of calpain-2 81290 3.4.22.53 acetyl-Leu-Leu-Nle-CHO complete inhibition at 0.001 mM 10273 3.4.22.53 acetyl-Leu-Leu-Nle-CHO broad spectrum calpain inhibitor 10273 3.4.22.53 acetyl-Leu-Leu-Nle-CHO - 10273 3.4.22.53 Al3+ inactivation at millimolar concentration of Ca2+ 264 3.4.22.53 ALLM - 40418 3.4.22.53 ALLN - 25515 3.4.22.53 alpha2-Macroglobulin 0.05 mg/ml, 11% inhibition 1068 3.4.22.53 antipain 0.01 mM, 80-90% inhibition 520 3.4.22.53 antipain 0.01 mM 56% inhibition 520 3.4.22.53 antipain 0.02 mM, 82% loss of activity 520 3.4.22.53 antipain 0.02 mM, 87% loss of activity 520 3.4.22.53 antipain - 520 3.4.22.53 antipain 0.05 mM, complete inhibition 520 3.4.22.53 benzyloxycarbonyl-L-leucyl-L-leucinal - 81302 3.4.22.53 benzyloxycarbonyl-Leu-Abu-CONH-CH2-C6H3(3,5-(OMe)2) calpain-2 selective inhibitor. A selective calpain-2 inhibitor could prevent acute glaucoma-induced retinal ganglion cell death and blindness 239887 3.4.22.53 benzyloxycarbonyl-Leu-Leu-leucinal - 113056 3.4.22.53 benzyloxycarbonyl-Leu-Leu-phenylalaninal - 111974 3.4.22.53 benzyloxycarbonyl-Leu-Leu-Tyr diazomethyl ketone - 113057 3.4.22.53 benzyloxycarbonyl-Leu-norleucinal - 113058 3.4.22.53 benzyloxycarbonyl-LLY-fluoromethylketone - 81308 3.4.22.53 Ca2+ initiation of autolysis of calpain 2 by adding of 1 mM CaCl2 15 3.4.22.53 Calmidazolium calpain-specific inhibitor 3621 3.4.22.53 calpain inhibitor I 0.002 mM, 95% loss of activity 12965 3.4.22.53 calpain inhibitor I 0.002 mM, 90% loss of activity 12965 3.4.22.53 calpain inhibitor I 0.05 mM, 99% inhibition 12965 3.4.22.53 calpain inhibitor II 0.002 mM, 67% loss of activity 16348 3.4.22.53 calpain inhibitor II 0.002 mM, 93% loss of activity 16348 3.4.22.53 calpain inhibitor II 0.05 mM, complete inhibition 16348 3.4.22.53 calpastatin - 1386 3.4.22.53 calpastatin inhibition of m-calpain is greater at pH 7.5 than at pH 6.5 at both 165 mM and 295 mM NaCl. Percentage inhibition is greater at 295 mM than at 165 mM NaCl 1386 3.4.22.53 calpastatin oxidation lowers calpastatin inhibition of m-calpain at al pH and ionic strength combinations 1386 3.4.22.53 calpastatin specific competitive inhibitor 1386 3.4.22.53 calpastatin endogenous inhibitor 1386 3.4.22.53 calpastatin endogenous inhibitor of calpain 1386 3.4.22.53 calpastatin specific inhibitor 1386 3.4.22.53 calpastatin II - 167879 3.4.22.53 calpeptin 50% inhibition of maximal caseinolytic activity at 10 nM and 21 nM for retinal and brain calpain 2399 3.4.22.53 calpeptin complete inhibition at 0.001 mM 2399 3.4.22.53 calpeptin Z-Leu-Nle-CHO 2399 3.4.22.53 calpeptin - 2399 3.4.22.53 caplastatin 2 - 113171 3.4.22.53 Cbz-Leu-DL-Abu-CONH-(CH2)3-(4-methylpiperazin-1-yl) - 86582 3.4.22.53 Cbz-Leu-DL-Abu-CONH-(CH2)3-2-methoxyadenin-9-yl - 86578 3.4.22.53 Cbz-Leu-DL-Abu-CONH-(CH2)3-adenin-9-yl - 86576 3.4.22.53 Cbz-Leu-DL-Abu-CONH-(CH2)3-cytosin-3-yl - 86580 3.4.22.53 Cbz-Leu-DL-Abu-CONH-(CH2)3-morpholine - 86575 3.4.22.53 CBZ-Leu-DL-Phe-CONH-(CH2)2-N-(CH3)2 - 86585 3.4.22.53 CBZ-Leu-DL-Phe-CONH-(CH2)3-(4-methylpiperazin-1-yl) - 86583 3.4.22.53 CBZ-Leu-DL-Phe-CONH-(CH2)3-2-methoxyadenin-9-yl - 86579 3.4.22.53 CBZ-Leu-DL-Phe-CONH-(CH2)3-adenin-9-yl best inhibitor 86577 3.4.22.53 CBZ-Leu-DL-Phe-CONH-(CH2)3-cytosin-3-yl - 86581 3.4.22.53 CBZ-Leu-DL-Phe-CONH-(CH2)3-N-(CH3)2 - 86584 3.4.22.53 Cd2+ 5 mM, inhibits in presence of 5 mM Ca2+ 52 3.4.22.53 Cd2+ 5 mM, completely blocks activation of the enzyme by Ca2+ 52 3.4.22.53 Cd2+ 5 mM 52 3.4.22.53 Co2+ 5 mM, inhibits in presence of 5 mM Ca2+ 23 3.4.22.53 Co2+ 5 mM, completely blocks activation of the enzyme by Ca2+ 23 3.4.22.53 Co2+ 5 mM 23 3.4.22.53 Co2+ 2.5 mM, strong 23 3.4.22.53 Cu2+ 5 mM, inhibits in presence of 5 mM Ca2+ 19 3.4.22.53 Cu2+ 5 mM, completely blocks activation of the enzyme by Ca2+ 19 3.4.22.53 Cu2+ 5 mM 19 3.4.22.53 E-64 0.05 mg/ml, complete inhibition 559 3.4.22.53 E-64 0.01 mM 89% inhibition 559 3.4.22.53 E-64 - 559 3.4.22.53 E-64 i.e. trans-epoxysuccinyl-L-leucylamido-(4-guanido)butane 559 3.4.22.53 E-64 0.01 mM, 98% inhibition 559 3.4.22.53 E-64c 0.01 mM, 80-90% inhibition 13400 3.4.22.53 EDTA 5 mM, complete inhibition 21 3.4.22.53 EDTA completely inactivated by 4 mM EDTA plus 4 mM EGTA 21 3.4.22.53 EGTA - 173 3.4.22.53 EGTA completely inactivated by 4 mM EDTA plus 4 mM EGTA 173 3.4.22.53 Ep-475 0.001 mM, 49% inhibition of the enzyme from retina, 46% inhibition of the enzyme from brain 8103 3.4.22.53 ethyl N-(phenylsulfonyl)-L-leucyl-L-phenylalaninate - 81304 3.4.22.53 Fe2+ 5 mM, inhibits in presence of 5 mM Ca2+ 25 3.4.22.53 Fe2+ 5 mM 25 3.4.22.53 Fe2+ 2.5 mM, strong 25 3.4.22.53 Fe3+ 5 mM 70 3.4.22.53 Fe3+ 2.5 mM, complete 70 3.4.22.53 GAP-43-3 a GAP-43 fragment, lacking about 40 N-terminal residues (named GAP-43-3), is produced by m-calpain-mediated cleavage of GAP-43. The fragment prevents complete cleavage of intact GAP-43 by m-calpain as a negative feedback. GAP-43-3 also blocks m-calpain activity against casein 37835 3.4.22.53 Hg2+ 5 mM, inhibits in presence of 5 mM Ca2+ 33 3.4.22.53 Hg2+ 5 mM 33 3.4.22.53 Hg2+ 2.5 mM, complete 33 3.4.22.53 indomethacin - 546 3.4.22.53 iodoacetamide 1 mM, 64% inhibition 67 3.4.22.53 iodoacetic acid 1 mM, 76% inhibition 213 3.4.22.53 iodoacetic acid 1 mM, complete loss of activity 213 3.4.22.53 iodoacetic acid 1 mM, 99% loss of activity 213 3.4.22.53 iodoacetic acid 0.1 mM, 99% inhibition 213 3.4.22.53 K+ inhibits at high concentrations 39 3.4.22.53 K+ 5 mM, inhibits in presence of 5 mM Ca2+ 39 3.4.22.53 leupeptin 0.05 mg/ml, complete inhibition 217 3.4.22.53 leupeptin 0.01 mM, 80-90% inhibition 217 3.4.22.53 leupeptin 0.01 mM 85% inhibition 217 3.4.22.53 leupeptin 0.001 mM, 67% inhibition of enzyme from retina and brain 217 3.4.22.53 leupeptin 0.002 mM, complete loss of activity 217 3.4.22.53 leupeptin 0.002 mM, 93% loss of activity 217 3.4.22.53 leupeptin - 217 3.4.22.53 leupeptin 0.05 mM, 99% inhibition 217 3.4.22.53 MDL-28170 - 11631 3.4.22.53 MDL28170 - 8857 3.4.22.53 MDL28170 selective calpain inhibitor 8857 3.4.22.53 Mg2+ 5 mM, inhibits in presence of 5 mM Ca2+ 6 3.4.22.53 Mn2+ 2.5 mM, strong 11 3.4.22.53 additional information suppression of calpain-2 expression with adenovirus vector-mediated RNAi 2 3.4.22.53 additional information specific capn2 shRNA reduces expression of the targeted isoform 2 3.4.22.53 additional information not inhibited by benzyloxycarbonyl-VAD-fluoromethylketone 2 3.4.22.53 additional information not inhibited by Ac-Thr-Pro-Leu-alpha-azaglycine-Ser-Pro-NH2, Ac-Pro-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2, Ac-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2, Ac-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2, Ac-Thr-Pro-Thr-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2, Ac-Thr-Pro-Leu-alpha-azaglycine-Ser-Ser-Pro-Pro-Ser-NH2, Ac-Thr-Pro-Leu-alpha-azaglycine-Ser-Gln-Pro-Pro-Ser-NH2, Ac-Thr-Pro-Val-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-NH2, Ac-Thr-Pro-Leu-alpha-azaglycine-Thr-Pro-Pro-Pro-Ser-NH2, and Ac-Thr-Pro-Leu-alpha-azaglycine-Arg-Pro-Pro-Pro-Ser-NH2 2 3.4.22.53 N-acetyl-L-leucyl-L-leucyl-L-methioninal - 160150 3.4.22.53 N-acetyl-Leu-Leu-Met - 160151 3.4.22.53 N-tosyl-Lys-chloromethyl ketone 0.5 mM, 69% inhibition 113978 3.4.22.53 N-tosyl-Phe-chloromethyl ketone 0.5 mM, 91% inhibition 112048 3.4.22.53 Na+ inhibits at high concentrations 59 3.4.22.53 Na+ 5 mM, inhibits in presence of 5 mM Ca2+ 59 3.4.22.53 NaCl m-calpain is more active at 165 mM NaCl than at 295 mM NaCl 42 3.4.22.53 NEM 3.0 mM, high inhibition of activity in presence or absence of Ca2+ 89 3.4.22.53 NEM 1 mM, 93% inhibition 89 3.4.22.53 NEM 5 mM, complete inhibition 89 3.4.22.53 Ni2+ 5 mM, inhibits in presence of 5 mM Ca2+ 38 3.4.22.53 Ni2+ 5 mM, completely blocks activation of the enzyme by Ca2+ 38 3.4.22.53 Ni2+ 5 mM 38 3.4.22.53 Ni2+ 2.5 mM, complete 38 3.4.22.53 NS-398 - 5807 3.4.22.53 PCMB 1 mM, 56% inhibition 78 3.4.22.53 PCMB 1 mM, 42% inhibition 78 3.4.22.53 PCMB 5 mM, 24% inhibition 78 3.4.22.53 PD150606 - 7903 3.4.22.53 pepstatin 0.01 mM, 99% inhibition 396 3.4.22.53 pepstatin A 1 mM, 60-80% inhibition 309 3.4.22.53 PMSF 1 mM, 6% inhibition 248 3.4.22.53 Polyethylene glycol PEG-4000, PEG-100000 or PEG-20000, inhibition at concentrations higher than 0.5% 2868 3.4.22.53 protease inhibitor 0.002 mg/ml, 6% inhibition 51889 3.4.22.53 SC-560 - 18639 3.4.22.53 SNJ-1945 - 40417 3.4.22.53 Thr-Pro-Leu-alpha-azaglycine-Ser-Pro-Pro-Pro-Ser-Pro-Arg-NH2 - 201837 3.4.22.53 TLCK 0.1 mM, 60-80% inhibition 4621 3.4.22.53 Z-Val-Phe-CHO i.e. MDL-28710m, 1.0 microM 63135 3.4.22.53 Zn2+ 5 mM, inhibits in presence of 5 mM Ca2+ 14 3.4.22.53 Zn2+ 5 mM, completely blocks activation of the enzyme by Ca2+ 14 3.4.22.53 Zn2+ 5 mM 14 3.4.22.53 Zn2+ 2.5 mM, complete 14