Suramin (sodium salt) [129-46-4]

Cat# HY-B0879A-50mg

Size : 50mg

Brand : MedChemExpress

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Description

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].

IC50 & Target[2]

SIRT1

297 nM (IC50)

SIRT2

1.15 μM (IC50)

SIRT5

22 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
J774 IC50
> 1000 μM
Compound: S2
Cytotoxicity against J774.1 cell line after 48 hrs
Cytotoxicity against J774.1 cell line after 48 hrs
[PMID: 16516467]
In Vitro

Suramin sodium salt (Suramin hexasodium salt; 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 sodium salt (300 μg/mL; for 48 hours) induces cells apoptosis and down-regulates mRNA expression in HeLa cells[7].
Suramin sodium salt (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.

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 hour
Result: Significantly suppressed the phosphorylated ERK1/2.
In Vivo

Suramin sodium salt (Suramin hexasodium salt; 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.

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
Molecular Weight

1429.17

Formula

C51H34N6Na6O23S6

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

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)

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (58.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (34.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6997 mL 3.4985 mL 6.9971 mL
5 mM 0.1399 mL 0.6997 mL 1.3994 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (1.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (1.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (69.97 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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