名称 | Suramin Sodium Salt |
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. |
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]. |
体外活性 | Suramin inhibits cell proliferation and DNA synthesis in cultured HeLa cells. The replication of SV40 DNA is completely abolished by 40 μM suramin. DNA polymerase α is sensitive to lower concentrations of suramin (IC50=8 μM) than is DNA polymerase δ (IC50=36 μM), whereas DNA polymerase β is relatively insensitive to the drug (IC50 of 90 μM)[1]. Suramin is a potent inhibitor of DNA strand exchange and ATPase activities of bacterial RecA proteins. Suramin inhibits RecA-catalysed proteolytic cleavage of the LexA repressor. The mechanism underlying such inhibitory actions of suramin involves its ability to disassemble RecA–single-stranded DNA filaments[2]. Suramin is a potent inhibitor of the nuclear enzyme DNA topoisomerase II. Suramin inhibits purified yeast topoisomerase II with an IC50 of about 5 μM[3]. |
体内活性 | Treatment with suramin shows lower values for pulmonary artery pressure, right ventricular hypertrophy, and distal vessel muscularization on day 21 compared to control rats. Suramin treatment suppresses PA-SMC proliferation and attenuates both the inflammatory response and the deposition of collagen[4]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (34.99 mM)
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关键字 | phosphatases | DNA | antiparasitic | Parasite | BAY 205 | anti-angiogenic | Phosphatase | Suramin Sodium Salt | Inhibitor | IP5K | Reverse Transcriptase | Apoptosis | Suramin hexasodium | anti-neoplastic | inhibit | NF060 | NF 060 | Topoisomerase | Sirtuin | protein-tyrosine | PTPases | SARS-CoV | Suramin | antitrypanosomal | SARS coronavirus | BAY205 |
相关产品 | Stavudine | Emtricitabine | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Lamivudine | Doxycycline | Tributyrin |
相关库 | 组蛋白修饰化合物库 | 经典已知活性库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 血管生成库 | 抗衰老化合物库 | 已知活性化合物库 | 磷酸酶抑制剂化合物库 | 抗癌药物库 | 抗癌活性化合物库 |