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 Broad-Spectrum Inhibitors of Proteolytic Enzyme Classes
Enzyme Explorer
 

Serine Protease Inhibitors
Cysteine Protease Inhibitors
Aspartic Protease Inhibitors
Metalloproteinase Inhibitors
References


Serine Protease Inhibitors
Product Code Inhibitor Characteristics Typical Working Concentration Prep. of Stock Solutions
L2884 Leupeptin Inhibits trypsin-like serine proteases such as trypsin, chymotrypsin, chymase, pepsin and thrombin. Inhibits selected cysteine proteases such as calpain, cathepsin B, H & L and papain. 10-100 µM 10 mM in water, stable 6 months at -20 °C
P7626 PMSF Broad spectrum serine protease inhibitor. Also reported to inhibit some cysteine proteases such as papain. 0.1-1.0 mM Prepare fresh in anhydrous ethanol or isopropanol at 200 mM
A8456 AEBSF Broad spectrum serine protease inhibitor. Also reported to inhibit some cysteine proteases such as papain. 0.1-1.0 mM 100 mM in water, stable 1 month at -20 °C
A1153 Aprotinin Does not inhibit thrombin or factor Xa. 0.3 µM or equimolar Freely soluble in water and stable at 2-8 °C
C7268 Chymostatin Inhibits chymotrypsin-like serine proteases such as chymase cathepsins A,B,D and G. Also inhibits some cysteine proteases such as papain. 10-100 µM 10 mM in DMSO, stable at -20 °C
A9141 Antithrombin III Inhibits thrombin, kallikreins, plasmin, trypsin and factors Ixa, Xa, and Xia equimolar Soluble at 10 un/ml in water, prepare stock solutions at neutral pH store at -20 °C
D7910 3,4-Dichloroisocoumarin Broad spectrum serine protease inhibitor 5-100 µM 10 mM in DMSO, stable at -20 °C
T7254 TLCK Inhibits trypsin-like serine proteases 10-100 µM Prepare fresh at 10 mM in 1 mM HCl
T4376 TPCK Inhibits chymotrypsin-like serine proteases 10-100 µM 10 mM in ethanol, stable at 4 °C
D0879 DIFP Highly toxic cholinesterase inhibitor. Broad spectrum serine protease inhibitor. Hydrolyzes rapidly in aqueous solutions 0.1 mM Prepare in anhydrous isopropanol at 200 mM
A6191 Antipain Inhibits serine proteases such as plasmin, thrombin and trypsin. Also inhibits some cysteine proteases such as calpain and papain. 1-100 µM 10 mM in water, stable 1 month at -20 °C
M6159 a2-Macroglobulin Broad spectrum protease inhibitor equimolar Water soluble, stable at -20 °C

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Cysteine Protease Inhibitors
Product Code Inhibitor Characteristics Typical Working Concentration Prep. of Stock Solutions
E3876 N-Ethylmaleimide Binds stoichiometrically to SH groups equimolar Water soluble at >10mg/ml, prepare fresh
L2884 Leupeptin Inhibits trypsin-like serine proteases such as trypsin, chymotrypsin, chymase, pepsin and thrombin. Inhibits selected cysteine proteases such as calpain, cathepsin B, H & L and papain. 10-100 µM 10 mM in water, stable 6 months at -20 °C
E3132 E-64 Will not inhibit serine protease with the exception of trypsin 1-10 µM 1 mM in water, stable at -20 °C
C7268 Chymostatin Inhibits chymotrypsin-like serine proteases such as chymase cathepsins A,B,D and G. Also inhibits some cysteine proteases such as papain 10-100 µM 10 mM in DMSO, stable at -20 °C
A6191 Antipain Inhibits serine proteases such as plasmin, thrombin and trypsin. Also inhibits some cysteine proteases such as calpain and papain. 1-100 µM 10 mM in water, stable 1 month at -20 °C
M6159 a2-Macroglobulin Broad spectrum protease inhibitor equimolar Water soluble, stable at -20 °C
P7626 PMSF Broad spectrum serine protease inhibitor. Also reported to inhibit some cysteine proteases such as papain. 0.1-1.0 mM Prepare fresh in anhydrous ethanol or isopropanol at 200 mM

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Aspartic Protease Inhibitors
Product Code Inhibitor Characteristics Typical Working Concentration Prep. of Stock Solutions
P5318 Pepstatin A Inhibits aspartic proteases such as renin, chymosin and pepsin 1 µM 1mM in methanol or DMSO, stable at -20 °C
M6159 a2-Macroglobulin Broad spectrum protease inhibitor equimolar Water soluble, stable at -20 °C

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Metalloproteinase Inhibitors
Product Code Inhibitor Characteristics Typical Working Concentration Prep. of Stock Solutions
ED2SS EDTA Broad spectrum metalloproteinase inhibitor 1-10 mM Very soluble and stable in water
P9375 1,10-Phenanthroline Broad spectrum metalloproteinase inhibitor 1-10 mM 200mM in methanol or DMSO, stable at -20 °C
R7385 Phosphoramidon Strong inhibitor of metalloendoproteinases, thermolysin and elastases, but a week inhibitor of collagenase 1-10 µM 1 mM in water, stable 1 month at -20 °C
B8385 Bestatin Inhibitor of aminopeptidases 1-10 µM 1 mM in methanol, stable 1 month at -20 °C
M6159 a2-Macroglobulin Broad spectrum protease inhibitor equimolar Water soluble, stable at -20 °C

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References
  1. Proteolytic Enzymes: A Practical Approach, R. J. Benyon and J. S. Bond, Eds, pp. 241-249 (1994)
  2. Handbook of Enzyme Inhibitors, 2nd ed, H. Zollner (1993)
  3. Sigma Data

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