Suramin 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1297.28

C₅₁H₄₀N₆O₂₃S₆

145-63-1

O=C(NC1=CC(C(NC2=CC(C(NC3=CC=C(S(=O)(O)=O)C4=CC(S(=O)(O)=O)=CC(S(=O)(O)=O)=C34)=O)=CC=C2C)=O)=CC=C1)NC5=CC(C(NC6=CC(C(NC7=CC=C(S(=O)(O)=O)C8=CC(S(=O)(O)=O)=CC(S(=O)(O)=O)=C78)=O)=CC=C6C)=O)=CC=C5

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

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]