3,4-Dichloroisocoumarin

3,4-Dichloroisocoumarin (3,4-DCI) is a serine protease inhibitor.¹ It completely inhibits enzyme activity of 24 serine proteases including human leukocyte elastase, thrombin, plasmin, Factor Xa, and Factor XIIa in vitro. 3,4-DCI stimulates caseinolytic activity of bovine pituitary multicatalytic proteinase complex (MPC) by inducing a conformational change in the MPC that exposes the caseinolytic active site.² It has been used to functionally characterize the catalytic activities of multiple proteases including rat liver MPC and extracellular lipase.^3,4

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1. Haper, J.W., Hemmi, K., and Powers, J.C. Reaction of serine proteases with substituted isocoumarins: Discovery of 3,4-dichloroisocoumarin, a new general mechanism based serine protease inhibitor. Biochemistry 24(8), 1831-1841 (1985).

2. Pereira, M.E., Nguyen, T., Wagner, B.J., et al. 3,4-dichloroisocoumarin-induced activation of the degradation of β-casein by the bovine pituitary multicatalytic proteinase complex. The Journal of Biological Chemisty 267(11), 7949-7955 (1992).

3. Djaballah, H., Harness, J.A., Savory, P.J., et al. Use of serine-protease inhibitors as probes for the different proteolytic activities of the rat liver multicatalytic proteinase complex. Eur. J. Biochem. 209(2), 629-634 (1992).

4. Ašler, I.L., Kovačić, F., Marchetti-Deschmann, M., et al. Inhibition of extracellular lipase from Streptomyces rimosus with 3,4-dichloroisocoumarin. J. Enzyme Inhib. Med. Chem. 28(5), 1094-1104 (2013).