The methanolic extract of the aerial parts of Persicaria thunbergii was found to show inhibitory activity on Farnesyl Protein Transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of isorhamnetin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the $IC_{50}$ value of isorhamnetin was $37.5;{mu}M$.