Suramin sodium salt

SKU:BHB21902667
Research Validated
Overview
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Suramin sodium salt (CAS 129-46-4) is an inhibitor supplied as a solid. Reported to act on SIRT1, SIRT2, SIRT5. Relevant to Metabolic Enzyme/Protease and Epigenetics research. Molecular formula C51H34N6Na6O23S6, molecular weight 1429.17 g/mol.
Purity 99.98%
CAS Number 129-46-4
Molecular Weight 1429.17 g/mol
Form Solid
Target SIRT1, SIRT2, SIRT5
Storage 4°C as supplied; in solvent -80°C
Options selector
Catalog no. Size
HY-B0879A-5MG 5 mg
HY-B0879A-10MG 10 mg
HY-B0879A-25MG 25 mg
HY-B0879A-50MG 50 mg
HY-B0879A-100MG 100 mg
HY-B0879A-200MG 200 mg
HY-B0879A-500MG 500 mg
HY-B0879A-1MLX10MM 1 mL x 10 mM (in DMSO)
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 mL x 10 mM (in DMSO)
  • Lead time: varies by selected option.
  • Storage: 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: refrigerate at 4°C as soon as possible.
Field Specification
Target SIRT1, SIRT2, SIRT5
Alternative names Suramin hexasodium salt
CAS no. 129-46-4
Applications
  • Functional Assay (In Vitro)
Molecular weight 1429.17
Molecular formula C51H34N6Na6O23S6
Purity 99.98%
SMILES 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
Form Solid
Storage 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-B0879A
Main SKU BHB21902667
Inhibitors

Compound Overview

Suramin sodium salt, also known as Suramin hexasodium salt, is a reversible, competitive inhibitor of protein-tyrosine phosphatases (PTPases)[1]. It is a potent inhibitor of the sirtuins SirT1 (IC50 = 297 nM), SirT2 (IC50 = 1.15 μM), and SirT5 (IC50 = 22 μM)[2], and a competitive inhibitor of reverse transcriptase, with an IC50 of 5 μM against DNA topoisomerase II[3][4]. It is also a potent inhibitor of the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp)[5], efficiently inhibits IP5K, and acts as an antiparasitic, anti-neoplastic, and anti-angiogenic agent[6][7][8]. It is supplied as an off-white to light brown solid (C51H34N6Na6O23S6, MW 1429.17) at 99.98% purity.

Physical & Chemical Properties

CAS Number 129-46-4
Molecular Formula C51H34N6Na6O23S6
Molecular Weight 1429.17 g/mol
Purity 99.98%
Appearance Solid
Color Off-white to light brown
SMILES 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
Target SIRT1, SIRT2, SIRT5
Signaling Pathway Metabolic Enzyme/Protease; Epigenetics; Cell Cycle/DNA Damage; Anti-infection; Apoptosis
Solubility In Vitro: DMSO: 50 mg/mL (34.99 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O: 50 mg/mL (34.99 mM; Requires sonication)
Storage 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
Shipping Room temperature in continental US; may vary elsewhere.

Biological Activity

IC50 & Target[2]

SIRT1

297 nM (IC50)

SIRT2

1.15 μM (IC50)

SIRT5

22 μM (IC50)

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[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]. 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.

[8]. 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.

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

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.

In Vitro

SolventSolubilityNotes
DMSO50 mg/mL (34.99 mM)requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility)
H2O50 mg/mL (34.99 mM)requires sonication

Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture and light; avoid repeated freeze-thaw cycles.

If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.

In Vivo

Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.

Protocol 1

Composition10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline
Result≥ 2.08 mg/mL (1.46 mM); clear solution
How to prepareGives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL.

Protocol 2

Composition10% DMSO + 90% (20% SBE-β-CD in saline)
Result≥ 2.08 mg/mL (1.46 mM); clear solution
How to prepareGives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week).

Direct preparation of the working solution

These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.

Protocol 3

CompositionPBS
Result100 mg/mL (69.97 mM); clear solution; requires sonication

Data provided by the manufacturer.

In Vitro

Cell proliferation is inhibited by Suramin sodium salt (Suramin hexasodium salt; 50-600 μg/mL; for 24-96 hours) in a dose- and time-dependent manner, and viability in cancer cells is decreased[7]. Suramin sodium salt (300 μg/mL; for 48 hours) induces cell apoptosis and downregulates mRNA expression in HeLa cells[7]. Phosphorylated ERK1/2 is significantly suppressed by Suramin sodium salt (1 mg/mL; 1 hour)[8]. The IC50 values for HO-8910 PM and HeLa are 319 μg/mL and 476 μg/mL, respectively[7]. Viral replication in Vero E6 cells is blocked by Suramin[5].

Cell Proliferation Assay[6]

Cell LineHO-8910 PM ovarian and Hela cervical cancer cells
Concentration50, 100, 200, 300, 400, 500 and 600 μg/mL
Incubation TimeFor 24, 48, 72 and 96 hours
ResultInhibited cells proliferation in a dose-dependent and time-dependent manner.

Apoptosis Analysis[6]

Cell LineHeLa cells
Concentration300 μg/mL
Incubation TimeFor 48 hours
ResultInduced cells apoptosis.

Western Blot Analysis[7]

Cell LinePA-SMCs cells
Concentration1 mg/mL
Incubation TimeFor 1 hour
ResultSignificantly suppressed the phosphorylated ERK1/2.

In Vivo

Established pulmonary hypertension (PH) is reversed by Suramin sodium salt (Suramin hexasodium salt; 10 mg/kg; IV; given twice weekly for 3 weeks), which normalizes pulmonary artery pressure values and vessel structure[8].

Animal ModelAdult male Wistar rats (200-225 g)[7]
Dosage10 mg/kg
AdministrationIV; twice weekly for 3 weeks
ResultReversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure.

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price on some sizes?
A.Availability and lead time for those sizes are confirmed on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat Struct Mol Biol 2021 Mar;28(3):319-325. PMID: 33674802

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