Here, by screening a bioactive compound library consisting of 429 small molecules, we identified for the first time that imperatorin, a naturally occurring furanocoumarin, exerted a most significantly inhibitory effect on TGFβ2 expression, and more importantly, markedly suppresses tumor invasion and metastasis in vitro and in vivo without overt side effects (Figure 2). This evidence concerns the gene TGFB2 and neoplasm.