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
- 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。
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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.
- 更新日期：2024/11/08
- 产品编号：HY-110137
- 产品名称：呋喃脒二盐酸盐 Furamidine dihydrochloride
- CAS编号：55368-40-6
- 包装：5mg
- 价格：1300元
- 更新日期：2024/11/08
- 产品编号：HY-110137
- 产品名称：呋喃脒二盐酸盐 Furamidine dihydrochloride
- CAS编号：
- 包装：10 mg
- 价格：2200元
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
