Among them, compound 1r (WCJ-394) was discovered to be a potent PRMT1 inhibitor, and the following studies showed that WCJ-394 significantly affected the expression of PRMT1-related proteins and inhibited the TGF-β1-induced EMT in A549 cells, which led to a significant inhibition on the cancer cells’ invasion and metastasis. This evidence concerns the gene TGFB1 and cancer.