苏拉明钠 T2160

Product Introduction
Bioactivity


英文名: Suramin Sodium Salt

描述: 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。

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

溶解度: DMSO : 50 mg/mL (34.99 mM)


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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途