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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 | In stock | |
5 mg | ¥ 1,070 | In stock | |
10 mg | ¥ 1,820 | In stock | |
25 mg | ¥ 3,930 | In stock | |
50 mg | ¥ 5,730 | In stock | |
100 mg | ¥ 7,750 | In stock | |
200 mg | ¥ 9,870 | In stock |
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 | PRMT5:166 µM (IC50), Protein arginine methyltransferase 1 (PRMT1):9.4 μM (IC50), PRMT4:>400 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. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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