| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Suramin sodium salt, a polysulfonated naphthylurea analog, is a novel and potent DNA topoisomerase II inhibitor with an IC50 of 5 μM. It has demonstrated various biological activities, for example, Suramin sodium is used as an antiparasitic drug. The mechanism of action for suramin is unclear, however, it is thought that parasites are able to selectively uptake suramin via receptor-mediated endocytosis of drug that is bound to low-density lipoproteins and to a lesser extent, other serum proteins. Once inside parasites, suramin combines with proteins, especially trypanosomal glycolytic enzymes to inhibit energy metabolism.
| ln Vitro |
In a dose-dependent and time-regulated manner, suramin sodium salt (also known as suramin hexasodium salt; 50-600 μg/mL; lasting 24-96 hours) suppresses cell proliferation and lowers lymphocyte viability [7]. mL; for 48 hours) causes HeLa cells to undergo apoptosis and express less mRNA [7]. One hour of 1 mg/mL suramin sodium salt suppresses phosphorylated ERK1/2 substantially [8]. HeLa and PM have IC50 values of 476 μg/mL and 319 μg/mL, respectively [7]. In Vero E6 cells, suramin sodium salt increases viral replication [5].
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| ln Vivo |
Suramin hexasodium salt (Suramin hexasodium salt; form 10 mg/kg; intravenously; twice weekly for 3 weeks) reverses established pulmonary hypertension (PH), consequently improving pulmonary artery pressure values and vascular structure Normal
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| Cell Assay |
Cell proliferation experiment[6]
Cell Types: HO-8910 PM ovarian cancer cells and HeLa cervical cancer cells Tested Concentrations: 50, 100, 200, 300, 400, 500 and 600 μg/mL Incubation Duration: 24, 48, 72 and 96 hrs (hours) Experimental Results: Cell proliferation was inhibited in a dose- and time-dependent manner. Apoptosis analysis [6] Cell Types: HeLa Cell Tested Concentrations: 300 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis. Western Blot Analysis[7] Cell Types: PA-SMCs Cell Tested Concentrations: 1 mg/mL Incubation Duration: 1 hour Experimental Results: Dramatically inhibited phosphorylated ERK1/2. |
| Animal Protocol |
Animal/Disease Models: Adult male Wistar rat (200-225 g) [7]
Doses: 10 mg/kg Route of Administration: IV; chemical [8]. Twice a week for 3 weeks Experimental Results:Reversal of established pH, thereby normalizing pulmonary artery pressure values and vascular structure. |
| 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. |
| Molecular Formula |
C51H34N6NA6O23S6
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|---|---|
| Molecular Weight |
1429.17
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| CAS # |
129-46-4
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| Related CAS # |
Suramin;145-63-1
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| SMILES |
O=C(NC1=CC(C(NC2=CC(C(NC(C(C3=CC(S([O-])(=O)=O)=C4)=C4S([O-])(=O)=O)=CC=C3S([O-])(=O)=O)=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.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
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| InChi Key |
VAPNKLKDKUDFHK-UHFFFAOYSA-H
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| InChi Code |
InChI=1S/C51H40N6O23S6.6Na/c1-25-9-11-29(49(60)54-37-13-15-41(83(69,70)71)35-21-33(81(63,64)65)23-43(45(35)37)85(75,76)77)19-39(25)56-47(58)27-5-3-7-31(17-27)52-51(62)53-32-8-4-6-28(18-32)48(59)57-40-20-30(12-10-26(40)2)50(61)55-38-14-16-42(84(72,73)74)36-22-34(82(66,67)68)24-44(46(36)38)86(78,79)80;;;;;;/h3-24H,1-2H3,(H,54,60)(H,55,61)(H,56,58)(H,57,59)(H2,52,53,62)(H,63,64,65)(H,66,67,68)(H,69,70,71)(H,72,73,74)(H,75,76,77)(H,78,79,80);;;;;;/q;6*+1/p-6
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| 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)
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| Synonyms |
NSC-34936l; NSC34936 ; NSC 34936;Suramin Hexasodium; BAY 205; BAY-205; BAY205; Germanin; NF 060; NF-060; NF060; Suramin; Farma; Fourneau;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~58.31 mM)
H2O : ~50 mg/mL (~34.99 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (1.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (1.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (69.97 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.0700 mL | 0.3499 mL | 0.6997 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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