Furamidine

Name: Furamidine
Brand: TargetMol
SKU: T11338
Rating: 4.5 (1 reviews)

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产品编号 T11338Cas号 73819-26-8

别名 NSC 305831, DB75

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

还可以

产品编号 T11338 别名 NSC 305831, DB75Cas号 73819-26-8

规格	价格	库存
25 mg	¥ 10,600	6-8周
50 mg	¥ 13,800	6-8周
100 mg	¥ 17,500	6-8周

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产品描述	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.
靶点活性	PRMT1:9.4 μM (IC50), PRMT6:283 µM (IC50), PRMT5:166 µM (IC50), PRMT4:>400 µM (IC50)
体外活性	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.
体内活性	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.
别名	NSC 305831, DB75