Biological Activity:

Furamidine is a potent, selective and cell permeable Protein arginine methyltransferase-1 (PRMT1) inhibitor with IC50 of 9.4 µM. It has >10-fold selectivity PRMT5, PRMT6 and CARM1 (IC50 are 166, 283 and >400 μM respectively). It targets the enzyme active site and is primarily competitive with the substrate and noncompetitive toward the cofactor. Furamidine effectively inhibits intracellular PRMT1 activity and blocks cell proliferation in leukemia cell lines with different genetic lesions.

How to Use:

In vitro: Furamidine was used at 10-30 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. (2014) J Med Chem. 57(6):2611-22.