73819-26-8

中文名称 4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)

CAS 73819-26-8

分子式 C18H16N4O

分子量 304.35

MOL 文件 73819-26-8.mol

73819-26-8 结构式

基本信息常见问题列表

基本信息

中文别名

呋喃脒

英文别名

NSC 305831
NSC 305831-d8
FuraMidine-d8
2,5-Bis(4-guanylphenyl)furan
2,5-bis(4-amidinophenyl)furan
2,5-Bis(4-guanylphenyl)furan-d8
2,5-Bis(4-aMidinophenyl)furan-d8
4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
Benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-
4-[5-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide

常见问题列表

生物活性

Furamidine (DB75) 是一种选择性的且细胞可渗透的蛋白精氨酸甲基转移酶 1 (PRMT1) 抑制剂，IC50 为 9.4 μM。Furamidine 对 PRMT1 的选择性高于 PRMT5，PRMT6 和 PRMT4 (CARM1) (IC50 分别为 166 µM，283 µM 和 >400 µM)。Furamidine 是一种有效的，可逆的和竞争性的酪氨酰 DNA 磷酸二酯酶 1 (TDP-1) 抑制剂。Furamidine 对 TDP-1 的抑制作用对单链和双链 DNA 底物均有效，对双链 DNA 的作用更强。Furamidine 也是一种抗寄生虫剂。

靶点

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

体外研究

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.
Furamidine (compound 1; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells.
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.

Cell Viability Assay

Cell Line:	Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
Concentration:	20 μM
Incubation Time:	72 hours
Result:	Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.

Western Blot Analysis

Cell Line:	293T cells
Concentration:	20 μM
Incubation Time:	15 hours
Result:	The expression level of the methylated GFP-ALY protein is significantly reduced.

体内研究

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.

Animal Model:	Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
Result:	Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.