Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA.

Furamidine binds duplex DNA in the DNA minor groove selectively at AT rich sites.?Furamidine can also intercalate between GC base pairs of duplex DNA.?Furamidine could therefore interfere with DNA processing enzymes such as TDP-1.Furamidine (; 20 μM; 72 hours; leukemia cell lines) inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations. Furamidine (; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells.

Furamidine (1 mg/kg;?intraperitoneal injection;?3 times a week and repeated every 4 weeks;?for 34 weeks;?female NZB/NZW mice) and Irinotecan combined treatment suppresses proteinuria and prolongs survival of lupus-prone NZB/NZW mice.?The combination treatment does not change the levels of anti-dsDNA antibodies.

73819-26-8

C18H16N4O

304.35

DB75;NSC 305831

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years