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Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K,是抗寄生虫,抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂,也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。
Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K,是抗寄生虫,抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂,也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 279 | 现货 | |
5 mg | ¥ 640 | 现货 | |
10 mg | ¥ 939 | 现货 | |
25 mg | ¥ 1,690 | 现货 | |
50 mg | ¥ 2,796 | 现货 | |
100 mg | ¥ 3,940 | 期货 |
产品描述 | Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis. |
靶点活性 | DNA topo II:5 μM |
体外活性 | Suramin 在培养的HeLa细胞中抑制细胞增殖和DNA合成。40 μM suramin 完全抑制了SV40 DNA的复制。与DNA聚合酶δ(IC50=36 μM)相比,DNA聚合酶α对较低浓度的suramin更敏感(IC50=8 μM),而DNA聚合酶β对该化合物相对不敏感(IC50=90 μM)[1]。Suramin是细菌RecA蛋白DNA链交换和ATP酶活性的强效抑制剂。Suramin抑制RecA催化的LexA抑制因子的蛋白水解切割。Suramin的抑制作用机制涉及其瓦解RecA-单链DNA丝的能力[2]。Suramin是核酶DNA拓扑异构酶II的强效抑制剂。Suramin抑制纯化的酵母拓扑异构酶II,其IC50约为5 μM[3]。 |
体内活性 | 与对照组大鼠相比,经Suramin处理后第21天的肺动脉压力、右心室肥大以及远端血管肌化指标均有所降低。Suramin的治疗能够抑制PA-SMC的增殖,并减轻炎症反应与胶原蛋白的沉积[4]。 |
激酶实验 | The ATPase assay is performed in a 10 μL reaction mixture containing 20 mM Tris-HCl (pH 7.5), 1 mM DTT, 8 mM MgCl2, 5 μM M13 circular ssDNA, 2.5 μM RecA from the specified bacterial species and increasing concentrations of suramin. The reaction is initiated by the addition of 2 mM [α-32P]ATP, incubated for 30 min at 37°C and stopped by the addition of 25 mM EDTA[2]. |
别名 | 苏拉明钠盐, 苏拉明钠, Suramin hexasodium salt, NF-060, BAY-205 |
分子量 | 1429.15 |
分子式 | C51H34N6Na6O23S6 |
CAS No. | 129-46-4 |
Smiles | [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].Cc1ccc(cc1NC(=O)c1cccc(NC(=O)Nc2cccc(c2)C(=O)Nc2cc(ccc2C)C(=O)Nc2ccc(c3cc(cc(c23)S([O-])(=O)=O)S([O-])(=O)=O)S([O-])(=O)=O)c1)C(=O)Nc1ccc(c2cc(cc(c12)S([O-])(=O)=O)S([O-])(=O)=O)S([O-])(=O)=O |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (34.99 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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