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CA-074, but Not Its Methyl Ester CA-074Me, Is a Selective Inhibitor of Cathepsin B Within Living Cells

CA-074, but Not Its Methyl Ester CA-074Me, Is a Selective Inhibitor of Cathepsin B Within Living Cells

Metwally Montaser, Gilles Lalmanach, Lukas Mach

Biol Chem. Jul-Aug 2002;383(7-8):1305-8.

PMID: 12437121

Abstract:

Studies using inhibitors that reportedly discriminate between cathepsin B and related lysosomal cysteine proteinases have implicated the enzyme in a wide range of physiological and pathological processes. The most popular substance to selectively inhibit cathepsin B in vivo is CA-074Me, the methyl ester of the E-64 derivative CA-074. However, we now have found that CA-074Me inactivates both cathepsin B and cathepsin L within murine fibroblasts. In contrast, exposure of these cells to the parental compound CA-074 leads to the selective inhibition of endogenous cathepsin B, while intracellular cathepsin L remains unaffected. These results indicate that CA-074 rather than CA-074Me should be used to specifically inactivate cathepsin B within living cells.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP134448105	CA-074		134448-10-5	Price

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