Pepstatin A is a competitive, reversible aspartic protease inhibitor and inhibits proteases such as pepsin, chymosin, renin, HIV proteases, and cathepsins D and E. It is highly selective and is often used in a mixture with other enzyme inhibitors. In vitro studies have shown pepstatin A is the only aspartic acid inhibitor that exhibits inhibitory effects on HIV proteases. Pepstatin A may also suppress differentiation of osteoclasts by inhibiting phosphorylation of MAP kinase and inhibiting NFATc1 expression. Pepstatin A has an application in cold inducible RNA-binding protein (CIRP) via CRISPR-Cas9 system. Pepstatin A inhibits lysosomal proteases directly.

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