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别名 呋喃脒二盐酸盐, NSC305831 dihydrochloride, NSC 305831 dihydrochloride, DB75 dihydrochloride
Furamidine dihydrochloride (DB75 dihydrochloride)是一种选择性的蛋白精氨酸甲基转移酶1(PRMT1)小分子抑制剂,可优先结合DNA小沟中的AT碱基对序列。Furamidine dihydrochloride主要通过与蛋白质底物竞争的方式靶向PRMT1酶活性位点(对辅因子为非竞争性抑制),在不同遗传背景的白血病细胞系中阻断细胞增殖。

Furamidine dihydrochloride (DB75 dihydrochloride)是一种选择性的蛋白精氨酸甲基转移酶1(PRMT1)小分子抑制剂,可优先结合DNA小沟中的AT碱基对序列。Furamidine dihydrochloride主要通过与蛋白质底物竞争的方式靶向PRMT1酶活性位点(对辅因子为非竞争性抑制),在不同遗传背景的白血病细胞系中阻断细胞增殖。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 445 | 现货 | |
| 5 mg | ¥ 1,070 | 现货 | |
| 10 mg | ¥ 1,820 | 现货 | |
| 25 mg | ¥ 3,930 | 现货 | |
| 50 mg | ¥ 5,730 | 现货 | |
| 100 mg | ¥ 7,750 | 现货 | |
| 200 mg | ¥ 9,870 | 现货 |
Furamidine dihydrochloride 相关产品
| 产品描述 | Furamidine dihydrochloride (DB75 dihydrochloride) is a cell-permeable, selective small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1) that also binds preferentially to strings of AT base pair sequences within the minor groove of DNA; it targets the PRMT1 enzyme active site primarily through a competitive mechanism with the protein substrate and is noncompetitive toward the cofactor, ultimately leading to the blockade of cell proliferation in various leukemia cell lines irrespective of their genetic lesions. |
| 靶点活性 | PRMT4:>400 µM (IC50), PRMT5:166 µM (IC50), Protein arginine methyltransferase 1 (PRMT1):9.4 μM (IC50), PRMT6:283 µM (IC50) |
| 体外活性 | Furamidine dihydrochloride (20 μM,72 小时) 处理白血病细胞系,其可以抑制除具有 JAK2V617F 突变的 HEL 细胞外的大多数白血病细胞系的细胞生长。[6] |
| 体内活性 | Furamidine dihydrochloride(1 mg/kg,腹腔注射,每周 3 次,每 4 周重复一次,共 34 周)处理雌性 NZB/NZW 小鼠,发现其联合伊立替康治疗可抑制蛋白尿,延长易患狼疮的 NZB/NZW 小鼠的生存期。[5] |
| 别名 | 呋喃脒二盐酸盐, NSC305831 dihydrochloride, NSC 305831 dihydrochloride, DB75 dihydrochloride |
| 分子量 | 377.27 |
| 分子式 | C18H18Cl2N4O |
| CAS No. | 55368-40-6 |
| Smiles | N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)N.Cl.Cl |
| 密度 | no data available |
| 存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | DMSO: 10 mg/mL (26.51 mM), Sonication is recommended. | |||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.65 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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