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Suramin hexasodium salt

Catalog No.: GC16832

Suramin hexasodium salt(Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor.

Suramin hexasodium salt Chemical Structure

Size Price Stock Qty
10mM (in 1mL DMSO)
$231.00
In stock
25mg
$210.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Vero E6 and Calu-3

Preparation Method

Vero E6 and Calu-3 cells were preincubated for 30 min with 2-fold serial dilutions of a starting concentration of 200 μM Suramin hexasodium salt and subsequently infected with 2 × 104 PFU of SARS-CoV-2 (MOI of 1 on Vero E6 cells) in 50 μl medium with compound.

Reaction Conditions

200μM for 16 hours or 21 hours

Applications

RT-qPCR revealed that the SARS-CoV-2 RNA levels decreased upon Suramin hexasodium salt treatment in a dose-dependent manner, showing a 3-log reduction at the highest concentration tested (200 μM)

Animal experiment [2]:

Animal models

C57BL/6JNarl (B6) mice

Preparation Method

Suramin hexasodium salt was diluted in normal saline, and indicated doses were administered at 4 h pre-infection, 1day post-infection or/and 3day post-infection (dpi) via the intraperitoneal (ip) route. Specifically, each dose comprised 0, 0.25, 0.5, 1 or 2 mg suramin hexasodium salt.

Dosage form

Intraperitoneal injection, 0, 0.25, 0.5, 1 or 2 mg

Applications

Viral loads in sera of mock-treated mice infected with the 0810bTw, 0611aTw and 0706aTw CHIKV strains at the 2 dpi peak were 5.8, 3 and 4.2 Log10 CCID50/ml, respectively (Fig. 2A). To parallel, viral titers of suramin hexasodium salt-treated sera after received two doses (pre 4 h and 1 dpi) were 5, 2.5 and 3.8 Log10 CCID50/ml for 0810bTw, 0611aTw and 0706aTw strains, respectively.

References:

[1]. Salgado-Benvindo, C., Thaler, M., Tas, A., Ogando, N. S., et al. Suramin inhibits SARS-CoV-2 infection in cell culture by interfering with early steps of the replication cycle. 2020. Antimicrob. Agents Chemother. 20, DOI: 10.1128/AAC.00900-20.

[2]. Kuo SC, Wang YM, Ho YJ, Chang TY, Lai ZZ, Tsui PY, Wu TY, Lin CC. 2016. Suramin treatment reduces chikungunya pathogenesis in mice. Antiviral Res 134:89–96.

Background

Suramin hexasodium salt is a polysulfonated naphthylurea with various biological activities. Suramin hexasodium salt is a DNA topoisomerase II inhibitor with an IC50 of 5 μM [1].

Suramin hexasodium salt at 300–600 μg/ml significantly inhibited HO-8910 PM and HeLa cell growth at 24 h, in both a time-dependent and dose-dependent manner, with an IC50 of 320 μg/ml and 475 μg/ml, respectively. Suramin hexasodium salt at 300 μg/ml significantly decreased the expression of Hpa mRNA (P < 0.005) and protein (P < 0.005) in both HO-8910 PM and HeLa cells at 48 h [2]. Suramin hexasodium salt shows antiviral activity against the newly emerged virus strain SARS-CoV-2 [3,4].Solution based assays of RdRp inhibition determined that the half-maximal inhibition concentration (IC50) of suramin hexasodium salt is 0.26 µM, Cell-based experiments indicated that suramin hexasodium salt was able to inhibit SARS-CoV-2 duplication in Vero E6 cells with a half-maximal effective concentration (EC50) of roughly 2.9 µM [3].Suramin hexasodium salt treatment of infected Vero E6 cells led to a reduction in extracellular viral RNA levels of up to 3 log. The highest concentration of compound that was used proved harmless to the cells; also, cytotoxicity was observed previously only above 5 mM. Suramin hexasodium salt also displayed antiviral efficacy in a human lung epithelial cell line, and we observed a >2 log reduction in levels of infectious virus progeny in suramin hexasodium salt -treated cells (CC50/EC90 = >55) [4].

Suramin hexasodium salt has therapeutic effects on CHIKV-infected mice. Suramin hexasodium salt treatment ameliorated foot swelling and reduced inflammatory infiltration, which corresponded to reduced viremia and viral antigen expression in infected tissues. Suramin hexasodium salt induces a dose-dependent reduction in foot swelling in CHIKV 0810bTw-infected mice, and the vary degrees of decreased viremia that was detected in suramin hexasodium salt -treated mice further confirmed therapeutic effects of this drug. In the time-related assay, a single dose of 2 mg suramin hexasodium salt (at 4 h pre-infection) or double doses of 2 mg suramin hexasodium salt (at 1 dpi and 3 dpi) significantly decreased disease score and viremia compared to mock-treated mice.

References:
[1]. Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.
[2]. Li, H.; Li, H.; Qu, H.; et al. Suramin inhibits cell proliferation in ovarian and cervical cancer by downregulating heparanase expression. Cancer Cell Int. 2015, 15, 1–11
[3]. Yin, W. et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat. Struct. Mol. Biol. 28, 319–325 (2021).
[4]. Salgado-Benvindo, C., Thaler, M., Tas, A., Ogando, N. S., et al. Suramin inhibits SARS-CoV-2 infection in cell culture by interfering with early steps of the replication cycle. 2020. Antimicrob. Agents Chemother. 20, DOI: 10.1128/AAC.00900-20
[5]. Kuo SC, Wang YM, Ho YJ, Chang TY, Lai ZZ, Tsui PY, Wu TY, Lin CC. 2016. Suramin treatment reduces chikungunya pathogenesis in mice. Antiviral Res 134:89–96.

Chemical Properties

Cas No. 129-46-4 SDF
Synonyms N/A
Chemical Name sodium 8,8'-((3,3'-((3,3'-(carbonylbis(azanediyl))bis(benzoyl))bis(azanediyl))bis(4-methylbenzoyl))bis(azanediyl))bis(naphthalene-1,3,5-trisulfonate)
Canonical SMILES [O-]S(=O)(C1=C(C(NC(C2=CC=C(C)C(NC(C3=CC=CC(NC(NC4=CC(C(NC5=CC(C(NC(C(C6=CC(S([O-])(=O)=O)=C7)=C7S([O-])(=O)=O)=CC=C6S([O-])(=O)=O)=O)=CC=C5C)=O)=CC=C4)=O)=C3)=O)=C2)=O)=CC=C8S([O-])(=O)=O)C8=CC(S([O-])(=O)=O)=C1)=O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
Formula C51H34N6Na6O23S6 M.Wt 1429.15
Solubility > 71.45mg/mL in Water; > 50mg/mL in DMSO Storage 4°C, protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Research Update

Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin

Nat Struct Mol Biol2021 Mar;28(3):319-325.PMID: 33674802DOI: 10.1038/s41594-021-00570-0

The COVID-19 pandemic caused by nonstop infections of SARS-CoV-2 has continued to ravage many countries worldwide. Here we report that suramin, a 100-year-old drug, is a potent inhibitor of the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) and acts by blocking the binding of RNA to the enzyme. In biochemical assays, suramin and its derivatives are at least 20-fold more potent than remdesivir, the currently approved nucleotide drug for treatment of COVID-19. The 2.6 Å cryo-electron microscopy structure of the viral RdRp bound to suramin reveals two binding sites. One site directly blocks the binding of the RNA template strand and the other site clashes with the RNA primer strand near the RdRp catalytic site, thus inhibiting RdRp activity. Suramin blocks viral replication in Vero E6 cells, although the reasons underlying this effect are likely various. Our results provide a structural mechanism for a nonnucleotide inhibitor of the SARS-CoV-2 RdRp.

Suramin

Cancer Pract1995 May-Jun;3(3):187-9.PMID: 7599677DOI: 10.1016/0305-7372(94)90003-5

In 2021, we commemorate the 40th anniversary of the identification of the disease AIDS, the acquired immune deficiency syndrome, a name that for the first time in history was launched in 1981 [...].

Suramin

Cancer Treat Rev1994 Jul;20(3):259-73.PMID: 8020006DOI: 10.1016/0305-7372(94)90003-5

In 2021, we commemorate the 40th anniversary of the identification of the disease AIDS, the acquired immune deficiency syndrome, a name that for the first time in history was launched in 1981 [...].

1984-Discovery of the First Anti-HIV Drug, Suramin

Viruses2021 Aug 19;13(8):1646.PMID: 34452510DOI: 10.3390/v13081646

In 2021, we commemorate the 40th anniversary of the identification of the disease AIDS, the acquired immune deficiency syndrome, a name that for the first time in history was launched in 1981 [...].

Targeted Redesign of Suramin Analogs for Novel Antimicrobial Lead Development

J Chem Inf Model2021 Sep 27;61(9):4442-4454.PMID: 34516120DOI: 10.1021/acs.jcim.1c00578

The emergence of new viral infections and drug-resistant bacteria urgently necessitates expedient therapeutic development. Repurposing and redesign of existing drugs against different targets are one potential way in which to accelerate this process. Suramin was initially developed as a successful antiparasitic drug but has also shown promising antiviral and antibacterial activities. However, due to its high conformational flexibility and negative charge, suramin is considered quite promiscuous toward positively charged sites within nucleic acid binding proteins. Although some suramin analogs have been developed against specific targets, only limited structure-activity relationship studies were performed, and virtual screening has yet to be used to identify more specific inhibitor(s) based on its scaffold. Using available structures, we investigated suramin's target diversity, confirming that suramin preferentially binds to protein pockets that are both positively charged and enriched in aromatic or leucine residues. Further, suramin's high conformational flexibility allows adaptation to structurally diverse binding surfaces. From this platform, we developed a framework for structure- and docking-guided elaboration of suramin analog scaffolds using virtual screening of suramin and heparin analogs against a panel of diverse therapeutically relevant viral and bacterial protein targets. Use of this new framework to design potentially specific suramin analogs is exemplified using the SARS-CoV-2 RNA-dependent RNA polymerase and nucleocapsid protein, identifying leads that might inhibit a wide range of coronaviruses. The approach presented here establishes a computational framework for designing suramin analogs against different bacterial and viral targets and repurposing existing drugs for more specific inhibitory activity.

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