中文名：苏拉明钠
CAS：129-46-4
品牌：MedChemExpress (MCE)
存储条件：4°C, sealed storage, away from moisture and light
生物活性：Suramin sodium salt (Suramin hexasodium salt) 是一种可逆的竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂[1]。 Suramin sodium salt 是 sirtuins 的有效抑制剂：SirT1 (IC50=297 nM)、SirT2 (IC50 =1.15 μM）和 SirT5（IC50=22 μM）[2]。苏拉明钠盐是逆转录酶的竞争性抑制剂（DNA 拓扑异构酶 II：IC50=5 μM）[3][4]。苏拉明钠盐是一种有效的SARS-CoV-2 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂[5]。苏拉明钠盐有效抑制 IP5K，是一种抗寄生虫、抗肿瘤和抗血管生成剂[6][7]。
体外：Suramin sodium salt (Suramin hexasodium salt; 50-600 μg/mL; for 24-96 hours) 以剂量依赖性和时间依赖性方式抑制细胞增殖并降低癌细胞的活力[7] .Suramin sodium salt (300 μg/mL; 48 h)诱导细胞凋亡，下调HeLa细胞的mRNA表达[7]。Suramin sodium salt (1 mg/mL; 1 hour) 显着抑制磷酸化的 ERK1/2[8]。HO-8910 PM和HeLa的IC50值分别为319 μg/mL、476 μg/mL[7]。苏拉明阻断 Vero E6 细胞中的病毒复制[5]。
体内：苏拉明钠盐（苏拉明六钠盐；10 mg/kg；静脉注射；每周两次，持续 3 周）可逆转已形成的肺动脉高压 (PH)，从而使肺动脉压力值和血管结构正常化[8]。
参考文献：[1]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.[2]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.[3]. Zhang YL, et al. Suramin is an active site-directed, reversible, and tight-binding inhibitor of protein-tyrosine phosphatases. J Biol Chem. 1998 May 15;273(20):12281-7.[4]. Trapp J, et al. Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins). ChemMedChem. 2007 Oct;2(10):1419-31.[5]. Schuetz A, et al. Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin. Structure. 2007 Mar;15(3):377-89.[6]. De Clercq E, et al. Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses. Cancer Lett. 1979 Nov;8(1):9-22.[7]. Novaes RD, et al. Purinergic Antagonist Suramin Aggravates Myocarditis and Increases Mortality by EnhancingParasitism, Inflammation, and Reactive Tissue Damage in Trypanosoma cruzi-Infected Mice. Oxid Med Cell Longev. 2018 Sep 30;2018:7385639.[8]. Wanchao Yin, et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat Struct Mol Biol. 2021 Mar;28(3):319-325.[9]. Xiaozhe Zhang, et al. Suramin and NF449 Are IP5K Inhibitors That Disrupt IP6-mediated Regulation of Cullin RING Ligase and Sensitize Cancer Cells to MLN4924/pevonedistat. J Biol Chem. 2020 Jun 3;jbc.RA120.014375.
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