Suramin (sodium salt)

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

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

[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.Br J Pharmacol. 2021 Aug 6.|Cell Metab. 2024 Sep 5:S1550-4131(24)00334-6.|J Agric Food Chem. 2023 Sep 19.|J Biol Chem. 2020 Jul 24;295(30):10281-10292. |J Biol Chem. 2021 Sep 3;101166.|J Med Chem. 2024 Jul 29.|J Virol Methods. 2021 Sep 14;298:114283.|Lipids Health Dis. 2023 Dec 13;22(1):222.|Nat Commun. 2024 Aug 27.|Nat Struct Mol Biol. 2021 Mar;28(3):319-325.|Research Square Preprint. 2020 Nov.|Behav Brain Res. 2023 Jun 22;114548.|Biomicrofluidics. 2019 Nov 21;13(6):064117.|Clin Transl Med. 2021 Jun;11(6):e485.|Int Immunopharmacol. 2023 May 12;120:110295.|J Bone Miner Metab. 2023 Jul 7.