Suramin sodium salt (Suramin hexasodium salt) is a reversible competitive protein tyrosine phosphatase (PTPases) inhibitor. Suramin sodium salt is an effective sirtuins inhibitor: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), SirT5 (IC50=22 μM). Suramin sodium salt is a competitive reverse transcriptase inhibitor (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt effectively inhibits IP5K and is an antiparasitic, antitumor and antiangiogenic agent.
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Biological activity
exterior
Suramin sodium salt (Suramin hexasodium salt; 50-600μg/mL; (24-96 hours) inhibits cell proliferation in a dose-dependent and time-dependent manner, and reduces the viability of cancer cells [6].
Suramin sodium salt (300 g/ml; induces apoptosis of HeLa cells [6] and down-regulates mRNA expression.
Suramin sodium salt (1 mg/ml; significantly inhibits phosphorylation of ERK1/2
The IC50 values of ho-8910pm and HeLa are 319°g/mL and 476°g/mL respectively
Cell proliferation test
Cell line: ho-8910pm ovarian cancer and Hela cervical cancer
Concentration: 50, 100, 200, 300, 400, 500, 600 mol/mL
Time: 24, 48, 72 and 96 hours
Results: The inhibition of cell proliferation was dose-dependent and time-dependent.
In the body
Suramin sodium (suramin hexa sodium; 10 mg/kg; fourth; 2 weeks for 3 weeks) reverses pulmonary hypertension (PH), thereby normalizing pulmonary artery pressure and vascular structure [7].
Animal model: adult male Wistar rat (200-225 g)
Dosage: 10 mg/kg
Method and frequency: fourth; twice a week for three weeks
Results: Reverse the established PH value, thereby normalizing the pulmonary artery pressure and vascular structure.