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4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
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- CAS号:
- 73819-26-8
- 英文名:
- 4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
- 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
- 中文名:
- 4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
- 中文别名:
- 呋喃脒;化合物 T11338
- CBNumber:
- CB31119955
- 分子式:
- C18H16N4O
- 分子量:
- 304.35
- MOL File:
- 73819-26-8.mol
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4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)化学性质
4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)性质、用途与生产工艺
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。
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)
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
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Cell Line:
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Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
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Concentration:
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20 μM
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Incubation Time:
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72 hours
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Result:
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Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.
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Western Blot Analysis
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Cell Line:
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293T cells
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Concentration:
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20 μM
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Incubation Time:
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15 hours
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Result:
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The expression level of the methylated GFP-ALY protein is significantly reduced.
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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.
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Animal Model:
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Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)
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Dosage:
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1 mg/kg
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Administration:
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Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
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Result:
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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)
上下游产品信息
上游原料
下游产品
4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)
生产厂家
73819-26-8, 4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide) 相关搜索:
- 化合物 T11338
- 呋喃脒
- 73819-26-8
- Benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-
- 4-[5-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide
- NSC 305831-d8
- FuraMidine-d8
- 2,5-Bis(4-guanylphenyl)furan-d8
- 2,5-Bis(4-aMidinophenyl)furan-d8
- NSC 305831
- 2,5-Bis(4-guanylphenyl)furan
- 2,5-bis(4-amidinophenyl)furan
- 4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide)