呋喃脒二盐酸盐

生物活性靶点体外研究体内研究呋喃脒二盐酸盐试剂级价格

呋喃脒二盐酸盐

CAS号:55368-40-6
英文名:Furamidine dihydrochloride
中文名:呋喃脒二盐酸盐
CBNumber:CB51518554
分子式:C18H16N4O
分子量:0
MOL File:55368-40-6.mol

呋喃脒二盐酸盐化学性质

熔点 :400-401 °C(Solv: ethanol (64-17-5))
储存条件 :-20°C
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :powder
颜色 :white to beige
稳定性 :Light Sensitive

呋喃脒二盐酸盐性质、用途与生产工艺

生物活性 Furamidine dihydrochloride (DB75 dihydrochloride) 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.