Description
General description
A competitive and reversible inhibitor of esterase and protease activity. Forms a tight complex with and blocks the active site of target enzymes. Inhibits a number of different proteases, including chymotrypsin, coagulation factors involved in the pre-phase of blood clotting, kallikrein (Kd = 1 X 10⁻⁷ M), plasmin (Kd = 2.3 X 10⁻¹⁰ M), tissue and leukocyte proteinases, and trypsin (Kd = 5 X 10⁻¹⁴ M). Does not inhibit Factor Xa or thrombin. Reported to be relatively acid and heat stable. Effectively inhibits target proteases at equimolar concentration. Useful as a serine proteinase inhibitor during purification of proteins and in studies of zymogen activation systems. Reported to suppress virus HA cleavage and limit reproduction of human and avian influenza viruses with a single arginine in the HA cleavage site.
Effectively inhibits target proteases at equimolar concentration.
Note: 1 KIU = 0.025 antiplasmin units (APU) = 0.0016 trypsin inhibitor units (using porcine trypsin) = 0.0009756 trypsin inhibitor units (using bovine trypsin).
Biochem/physiol Actions
Kd = 1 x 10-7 M, 2.3 x 10-10 M, 5 x 10-14 M, against kallikrein, plasmin, and trypsin, respectively
Primary Target
chymotrypsin
Preparation Note
Following reconstitution refrigerate (4°C). Stock solutions are stable for up to 3 months at 4°C.
Other Notes
One Kallikrein Inhibitory Unit (K.I.U.) is defined as the quantity of protease inhibitor that will inhibit two kallikrein units by 50% under optimal conditions. Note: 1 KIU = 0.025 antiplasmin units (APU) or 0.0031 trypsin inhibitor units.
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Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)