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| Molecular weight | |
| Molecular formula | C51H40N6O23S6 |
| SMILES | |
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Compound Overview
Suramin 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 has the molecular formula C51H40N6O23S6 and a molecular weight of 1297.28 g/mol.
Physical & Chemical Properties
| CAS Number | 145-63-1 |
|---|---|
| Molecular Formula | C51H40N6O23S6 |
| Molecular Weight | 1297.28 g/mol |
| 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 |
| Target | SIRT1, SIRT2, SIRT5 |
| Signaling Pathway | Metabolic Enzyme/Protease; Epigenetics; Cell Cycle/DNA Damage; Anti-infection; Apoptosis |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Cell proliferation is inhibited by Suramin (50-600 μg/mL; for 24-96 hours) in a dose- and time-dependent manner, and viability in cancer cells is decreased[7]. Suramin (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 (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 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 hours |
| Result | Significantly suppressed the phosphorylated ERK1/2. |
In Vivo
Established pulmonary hypertension (PH) is reversed by Suramin (10 mg/kg; IV; twice weekly for 3 weeks), which normalizes pulmonary artery pressure values and vessel structure[8].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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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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Suramin, an antiparasitic drug, stimulates adipocyte differentiation and promotes adipogenesis. Lipids Health Dis 2023 Dec 13;22(1):222. PMID: 38093311
