Suramin(Synonyms: 苏拉明)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Suramin (Synonyms: 苏拉明)

Suramin 是一种可逆的，竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。Suramin 是有效的 sirtuins 抑制剂：SirT1 (IC50=297 nM)，SirT2 (IC50=1.15 μM)，SirT5 (IC50=22 μM)。Suramin 是竞争性逆转录酶抑制剂 (DNA topoisomerase II: IC50=5 μM)。Suramin 是一种有效的 SARS-CoV-2 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。Suramin 有效抑制 IP5K，并且是抗寄生虫 (antiparasitic)，抗肿瘤和抗血管生成剂。

Suramin(Synonyms: 苏拉明)

Suramin Chemical Structure

CAS No. : 145-63-1

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Suramin 的其他形式现货产品:

Suramin sodium salt

生物活性

Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor[1]. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM)[2]. Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM)[3][4]. Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor[5].Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent[6][7][8].

IC50 & Target[2]

SIRT1

297 nM (IC50)

SIRT2

1.15 μM (IC50)

SIRT5

22 μM (IC50)

体外研究
(In Vitro)

Suramin (50-600 μg/mL; for 24-96 hours) inhibits cells proliferation in a dose-dependent and time-dependent manner and decreases viability in cancer cells[7].
Suramin (300 μg/mL; for 48 hours) induces cells apoptosis, and down-regulates mRNA expression in HeLa cells[7].
Suramin (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2[8].
The IC50 values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively[7].
Suramin blocks viral replication in Vero E6 cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[6]

Cell Line: HO-8910 PM ovarian and Hela cervical cancer cells
Concentration: 50, 100, 200, 300, 400, 500 and 600 μg/mL
Incubation Time: For 24, 48, 72 and 96 hours
Result: Inhibited cells proliferation in a dose-dependent and time-dependent manner.

Apoptosis Analysis[6]

Cell Line: HeLa cells
Concentration: 300 μg/mL
Incubation Time: For 48 hours
Result: Induced cells apoptosis.

Western Blot Analysis[7]

Cell Line: PA-SMCs cells
Concentration: 1 mg/mL
Incubation Time: For 1 hours
Result: Significantly suppressed the phosphorylated ERK1/2.

体内研究
(In Vivo)

Suramin (10 mg/kg; IV; twice weekly for 3 weeks) reverses established pulmonary hypertension (PH), thereby normalizing the pulmonary artery pressure values and vessel structure[8].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male Wistar rats (200-225 g)[7]
Dosage: 10 mg/kg
Administration: IV; twice weekly for 3 weeks
Result: Reversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure.

Clinical Trial

分子量

1297.28

Formula

C51H40N6O23S6
CAS 号

145-63-1
中文名称

苏拉明
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. 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.

    [2]. 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.

    [3]. Schuetz A, et al. Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin. Structure. 2007 Mar;15(3):377-89.

    [4]. 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.

    [5]. 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.

    [6]. 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.

    [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]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.

    [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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