N-[3-(4-hydroxyphenyl)-1-oxo-2-propenyl]-L-phenylalanine, methyl ester, inhibits human Acyl-Coenzyme A cyltransferase-1 and -2 (ACAT-1 and ACAT-2) equally (IC50 ~ 60 μM). ACAT-1 and ACAT-2 catalyze the formation of long chain fatty acyl-coenzyme A and cholesterol esters from cholesterol, and may play a role in the development of atherosclerosis. Additionally, at a concentration of 3μM, N-[3-(4-hydroxyphenyl)-1-oxo-2-propenyl]-L-phenylalanine, methyl ester, demonstrates ~28% inhibition of copper-mediated oxidation of low density lipoproteins.