Suramin 是一种可逆的,竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。Suramin 是有效的sirtuins抑制剂:SirT1 (IC50=297 nM),SirT2 (IC50=1.15 μM),SirT5 (IC50=22 μM)。Suramin 是竞争性逆转录酶抑制剂 (DNA topoisomerase II:IC50=5 μM)。Suramin 是一种有效的 SARS-CoV-2 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。Suramin 有效抑制IP5K,并且是抗寄生虫 (antiparasitic),抗肿瘤和抗血管生成剂。
生物活性 | Suramin is a reversible and competitiveprotein-tyrosine phosphatases (PTPases)inhibitor[1]. Suramin is a potent inhibitor ofsirtuins:SirT1(IC50=297 nM),SirT2(IC50=1.15 μM), andSirT5(IC50=22 μM)[2]. Suramin is a competitive inhibitor ofreverse transcriptase(DNAtopoisomeraseII:IC50=5 μM)[3][4]. Suramin is a potentSARS-CoV-2 RNA-dependent RNA polymerase (RdRp)inhibitor[5].Suramin efficiently inhibitsIP5Kand is anantiparasitic, 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) |
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体外研究 (In Vitro) | Suramin (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 (300 μg/mL; for 48 hours) induces cells apoptosis, and down-regulates mRNA expression in HeLa cells[7]. Suramin (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2[8]. The IC50values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively[7]. Suramin blocks viral replication in Vero E6 cells[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. |
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体内研究 (In Vivo) | Suramin (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].
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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |