Furamidine is a cell-permeable, selective inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine targets the enzyme active site and is primarily competitive with the substrate and noncompetitive toward the cofactor. Furthermore, Furamidine blocks cell proliferation in leukemia cell lines with different genetic lesions.