Suramin sodium salt (Suramin hexasodium salt) 是一种可逆的竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。Suramin sodium salt 是有效的sirtuins抑制剂：SirT1 (IC50=297 nM)，SirT2 (IC50=1.15 μM)，SirT5 (IC50=22 μM)。Suramin sodium salt 是竞争性逆转录酶抑制剂 (DNA topoisomerase II:IC50=5 μM)。Suramin sodium salt 是一种有效的 SARS-CoV-2 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。Suramin sodium salt 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 sodium salt (Suramin hexasodium salt) is a reversible and competitiveprotein-tyrosine phosphatases (PTPases)inhibitor[1]. Suramin sodium salt is a potent inhibitor ofsirtuins:SirT1(IC50=297 nM),SirT2(IC50=1.15 μM), andSirT5(IC50=22 μM)[2]. Suramin sodium salt is a competitive inhibitor ofreverse transcriptase(DNAtopoisomeraseII:IC50=5 μM)[3][4]. Suramin sodium salt is a potentSARS-CoV-2 RNA-dependent RNA polymerase (RdRp)inhibitor[5]. Suramin sodium salt 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 sodium salt (Suramin hexasodium salt; 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 sodium salt (300 μg/mL; for 48 hours) induces cells apoptosis and down-regulates mRNA expression in HeLa cells[7].
Suramin sodium salt (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 hour | | Result: | Significantly suppressed the phosphorylated ERK1/2. |
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体内研究
(In Vivo) | Suramin sodium salt (Suramin hexasodium salt; 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 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(69.97 mM;Need ultrasonic) DMSO : 83.33 mg/mL(58.31 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (69.97 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (1.46 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (1.46 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (1.46 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (1.46 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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