Furamidine (DB75) is a selectiveprotein arginine methyltransferase 1 (PRMT1)inhibitor with anIC₅₀of 9.4 μM. Furamidine is selective forPRMT1overPRMT5,PRMT6, andPRMT4(CARM1) (IC₅₀s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine is a potent, reversible and competitivetyrosyl-DNAphosphodiesterase1 (TDP-1)inhibitor. Inhibition ofTDP-1by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent^[1][2][3].

IC50: 9.4 μM (Protein arginine methyltransferase 1 (PRMT1)); 166 μM (PRMT5), 283 μM (PRMT6) and >400 μM (PRMT4)^[1]
Parasite^[1]
Tyrosyl-DNA phosphodiesterase 1 (TDP-1)^[2]

Furamidine (compound 1; 20 μM; 72 hours; leukemia cell lines) inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations^[1].
Furamidine (compound 1; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells^[1].
Furamidine binds duplex DNA in the DNA minor groove selectively at AT rich sites [(A/T)4]. Furamidine can also intercalate between GC base pairs of duplex DNA. Furamidine could therefore interfere with DNA processing enzymes such as TDP-1^[2].

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^[3].

304.35

C₁₈H₁₆N₄O

73819-26-8

呋喃脒

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.