Two cathepsin B inhibitory peptides were isolated from a commercial pancreatic digest of casein. The peptides were identified as the Pro-Phe-Pro-Gly-Pro-Ile and the Gly-Pro-Phe-Pro-Ile corresponding to the sequence 61-66 and 203-207 of bovine beta-casein. These peptides showed competitive inhibition for cathepsin B with the K(i) values of 2.31 and 3.30 mM, respectively. Two related analogues, Tyr-Pro-Phe-Pro-Gly-Pro-Ile and Val-Tyr-Pro-Phe-Pro-Gly-Pro-Ile, were synthesized but their cathepsin B inhibitory activity was not detected.