Furamidine (hydrochloride) (DB75 dihydrochloride) 是一种选择性蛋白质精氨酸甲基转移酶 1 (PRMT1) 抑制剂，IC50 为 9.4 μM.
| Cas No. | 55368-40-6 |
| 别名 | 呋喃脒二盐酸盐,DB75 dihydrochloride; NSC 305831 dihydrochloride |
| Canonical SMILES | NC(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)=N.Cl.Cl |
| 分子式 | C18H16N4O•2HCl |
| 分子量 | 377.3 |
| 溶解度 | DMF: 0.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): Partially soluble |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
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描述 | Furamidine is a cell-permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) that is selective for PRMT1 over PRMT5, PRMT6, and PRMT4/coactivator-associated arginine methyltransferase 1 (CARM1) (IC50s = 9.4, 166, 283, and >400 μM, respectively). In vitro, furamidine (20 μM) inhibits Aly protein methylation in HEK293T cells and growth of several leukemia cell lines. It inhibits tyrosyl-DNA phosphodiesterase (Tdp1) activity on both single- and double-stranded DNA substrates with concentrations in the low micromolar range, but it is more potent against a duplex DNA substrate. Furamidine inhibits growth of T. brucei, the parasite that causes sleeping sickness, with IC50 values of 1.5 to 37 nM across various strains. It inhibits the T. brucei P2 aminopurine transporter (Ki = 1.2 μM). It also binds to AT-rich DNA sequences in trypanosome kinetoplast DNA. |
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