E-64c

E-64c is an active metabolite of the protease inhibitor E-64d (Item No. 13533).^1,2,3,4 E-64c inhibits the cysteine proteases cathepsin B, cathepsin H, and papain but not the serine proteases trypsin, chymotrypsin, or elastase.^5,6 It reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease when used at concentrations ranging from 0.1 to 1 mg/ml.³ E-64c reduces infection of HEK293T cells by an HIV-based virus system pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) surface glycoprotein, also known as the spike glycoprotein, in a concentration-dependent manner.⁴

WARNING This product is not for human or veterinary use.

1. Shoji, Y., Senshu, M., Iwashita, S., et al. Thiol protease-specific inhibitor E-64 arrests human epidermoid carcinoma A431 cells at mitotic metaphase. Proc. Natl. Acad. Sci. USA 85(1), 146-150 (1988).

2. Roush, W.R., Hernandez, A.A., McKerrow, J.H., et al. Design, synthesis and evaluation of d-homophenylalanyl epoxysuccinate inhibitors of the trypanosomal cysteine protease cruzain. Tetrahedron 56(50), 9747-9762 (2000).

3. Kleina, L.G., and Grubman, M.J. Antiviral effects of a thiol protease inhibitor on foot-and-mouth disease virus. J. Virol. 66(12), 7168-7175 (1992).

4. Simmons, G., Gosalia, D.N., Rennekamp, A.J., et al. Inhibitors of cathepsin L prevent severe acute respiratory syndrome coronavirus entry. Proc. Natl. Acad. Sci. USA 102(33), 11876-11881 (2005).

5. Barrett, A.J., Kembhavi, A.A., Brown, M.A., et al. L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L. Biochem. J. 201(1), 189-198 (1982).

6. Tamai, M., Matsumoto, K., Omura, S., et al. In vitro and in vivo inhibition of cysteine proteinases by EST, a new analog of E-64. J. Pharmacobiodyn. 9(8), 672-677 (1986).