| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| 250mg | ||
| 500mg |
Suramin, 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 |
Suramin (50-600 μg/mL; for 24-96 hours) suppresses cell growth and lowers cancer cell viability in a dose- and time-dependent manner [7]. Suramin (300 μg/mL; for 48 hours) causes apoptosis and downregulates mRNA expression in HeLa cells [7]. Suramin (1 mg/mL; 1 hour) effectively suppresses phosphorylated ERK1/2 [8]. The IC50 values of HO-8910 PM and HeLa are 319 μg/mL and 476 μg/mL respectively [7]. Suramin suppresses viral replication in Vero E6 cells [5].
|
|---|---|
| ln Vivo |
Suramin (10 mg/kg; intravenously administered twice weekly for three weeks) normalizes pulmonary artery pressure values and vascular structure by reversing established pulmonary hypertension (PH) [8].
|
| Cell Assay |
Cell proliferation assay[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: intravenous (iv) (iv)injection; twice a week for 3 weeks Experimental Results: Reversal of established PH, thereby increasing pulmonary artery pressure values and normalization of vascular structures. |
| 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]. 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]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073. [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. |
| Molecular Formula |
C51H40N6O23S6
|
|---|---|
| Molecular Weight |
1297.2797
|
| CAS # |
145-63-1
|
| Related CAS # |
Suramin sodium salt;129-46-4
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
O=C(NC1=CC(C(NC2=CC(C(NC3=CC=C(S(=O)(O)=O)C4=CC(S(=O)(O)=O)=CC(S(=O)(O)=O)=C34)=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
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7708 mL | 3.8542 mL | 7.7084 mL | |
| 5 mM | 0.1542 mL | 0.7708 mL | 1.5417 mL | |
| 10 mM | 0.0771 mL | 0.3854 mL | 0.7708 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
