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ChemicalBook  CAS数据库列表  4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)

4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)

生物活性 靶点 体外研究 体内研究
4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide),73819-26-8,结构式
4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
  • CAS号:73819-26-8
  • 英文名:4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
  • 中文名:4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
  • CBNumber:CB31119955
  • 分子式:C18H16N4O
  • 分子量:304.35
  • MOL File:73819-26-8.mol

4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)性质、用途与生产工艺

  • 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.
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4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)生产厂家
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