货号:A397022
同义名:
苏拉明钠盐
/ Suramin hexasodium salt; Suramin Sodium
Suramin sodium salt (Suramin hexasodium salt) 是一种可逆的、竞争性的蛋白酪氨酸磷酸酶(PTPases)抑制剂。它是一种有效的sirtuins抑制剂:SirT1(IC50=297 nM)、SirT2(IC50=1.15 μM)和SirT5(IC50=22 μM),并且还作为一种逆转录酶的竞争性抑制剂(DNA拓扑异构酶II:IC50=5 μM)。苏拉明钠盐是一种有效的SARS-CoV-2 RNA依赖的RNA聚合酶(RdRp)抑制剂,并有效抑制IP5K。此外,它具有抗寄生虫、抗肿瘤和抗血管生成特性。


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| 靶点 |
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| 描述 | Suramin sodium salt is a polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors(10-100 μM). |
| Concentration | Treated Time | Description | References | |
| Saos-2 cells | 10 –25 µM | 6 weeks | No telomere shortening was observed | AAPS J. 2015 Jan;17(1):268-76. |
| DU145 cells | 300 µg/ml | 10 minutes | To determine the effects of suramin on tyrosine phosphorylation in DU145 cells, it was found that suramin significantly increased the tyrosine phosphorylation of 75 and 135 kDa proteins. | J Clin Invest. 1992 Dec;90(6):2166-74. |
| LNCaP cells | 300 µg/ml | 10 minutes | To determine the effects of suramin on tyrosine phosphorylation in LNCaP cells, it was found that suramin significantly increased the tyrosine phosphorylation of 75 and 135 kDa proteins. | J Clin Invest. 1992 Dec;90(6):2166-74. |
| Lycopersicon peruvianum suspension-cultured cells | 700 µM | 10 minutes | Suramin inhibited the alkalinization of the medium induced by systemin, chitosan, and pmg elicitor. | Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):8862-7. |
| Monocytes | 200 µM | 2 days | Suramin reduced the expression of FcγRI, FcγRII, FcεRII, and FcαR on monocytes and impaired their phagocytic capacity. | Immunology. 1994 Apr;81(4):598-604. |
| Chinese hamster fibrosarcoma cells (DC-3F) | 50 µM | 24 hours | Determine the intracellular distribution of Suramin, results showed Suramin was predominantly located in the nucleus. | Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9. |
| KB cells | 300 µM | 24 hours and 48 hours | To investigate the effect of Suramin on the growth of KB cells, results showed that Suramin was able to sustain the growth of KB carcinoma cells cultured under serum-free conditions. | J Clin Invest. 1992 Apr;89(4):1242-7. |
| HEK293T cells | 0.02 - 5 mM | 4 hours | To evaluate the neutralizing effect of Suramin on SARS-CoV-2 pseudotyped viral particles, results showed that Suramin exhibited broad entry inhibition among all three variants tested (wild type, Delta, and Omicron) | Commun Biol. 2023 Apr 8;6(1):387. |
| Vero E6 cells | 5, 10, 50, 100, 1000, 10000 µM | 48 hours | To evaluate the cytotoxicity of Suramin on Vero E6 cells, results showed very low cytotoxicity (<20%) even at suramin concentrations up to 10 mM | Commun Biol. 2023 Apr 8;6(1):387. |
| Lycopersicon peruvianum suspension-cultured cells | 1 mM | 5 minutes | Suramin inhibited the activation of the 48-kDa MBP kinase induced by systemin, chitosan, and pmg elicitor. | Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):8862-7. |
| FaDu cells | 10 –25 µM | 6 weeks | Inhibited telomerase activity, leading to gradual telomere shortening (maximum of 30%) and cell senescence | AAPS J. 2015 Jan;17(1):268-76. |
| PC3 cells | 10 –25 µM | 6 weeks | Inhibited telomerase activity, leading to gradual telomere shortening (maximum of 30%) and cell senescence | AAPS J. 2015 Jan;17(1):268-76. |
| MCF7 cells | 10 –25 µM | 6 weeks | Inhibited telomerase activity, leading to gradual telomere shortening (maximum of 30%) and cell senescence | AAPS J. 2015 Jan;17(1):268-76. |
| A431 cells | 100 µM and 300 µM | 72 hours and 96 hours | To investigate the effect of Suramin on EGFR in A431 cells, results showed that Suramin treatment led to a dramatic reduction in EGFR abundance and a shift in EGFR mobility, indicating Suramin-induced downregulation of EGFR. | J Clin Invest. 1992 Apr;89(4):1242-7. |
| U937 cells | 50-200 µM | 8-72 hours | Suramin inhibited the proliferation of U937 cells and reduced the expression of FcγRI, FcγRII, FcεRII, and FcαR. | Immunology. 1994 Apr;81(4):598-604. |
| U-266 cells | 30 µM | 90 minutes | Suramin inhibited the binding of 125I-IL-6 to U-266 cells, with a half-maximal inhibition concentration of 30 μM | J Clin Invest. 1993 Nov;92(5):2152-9. |
| MCF-7 cells | 300 µM | 90 minutes | Suramin inhibited the binding of 125I-TNFα to MCF-7 cells, with a half-maximal inhibition concentration of 300 μM | J Clin Invest. 1993 Nov;92(5):2152-9. |
| PC3 cells | 300 µg/ml | seconds | To determine the effects of suramin on tyrosine phosphorylation in PC3 cells, it was found that suramin significantly increased the tyrosine phosphorylation of several distinct proteins. | J Clin Invest. 1992 Dec;90(6):2166-74. |
| U2OS cells | 62.5 to 500 µM | Suramin at 62.5 μM accumulated p27 and CDT1, and at 250-500 μM accumulated Nrf2, indicating that Suramin inhibits CRL-mediated ubiquitination, leading to the accumulation of CRL substrates. | Proc Natl Acad Sci U S A. 2016 Apr 5;113(14):E2011-8. | |
| B-9 cells | 30 µM | Suramin inhibited the proliferation of B-9 cells in response to IL-6, with a half-maximal inhibition concentration of 30 μM | J Clin Invest. 1993 Nov;92(5):2152-9. | |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | FaDu tumor model | Intravenous injection | 10 mg/kg | Twice a week for 6 weeks | Resulted in telomere shortening of >40% in tumor cells | AAPS J. 2015 Jan;17(1):268-76. |
| Mice | Pkd1-deficient mouse model | Intraperitoneal injection | 60 mg/kg | Twice a week for 8 weeks | Suramin significantly reduced renal cyst densities, cell proliferation, and macrophage infiltration, but did not improve kidney function | Int J Mol Sci. 2022 Jul 31;23(15):8499 |
| Tomato plants | 14-day-old tomato plants | Supplied through cut stems | 700 µM | 1-hour pretreatment | Suramin inhibited the synthesis of serine proteinase inhibitors I and II induced by systemin and completely inhibited the synthesis of inhibitors induced by wounding. | Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):8862-7. |
| BALB/c X DBA/2 (CD)F1 mice | C-26 adenocarcinoma model | Intraperitoneal injection | 75 mg/kg | Injected on days 7 and 12 | Suramin significantly improved weight loss in C-26 adenocarcinoma model mice, reducing muscle and fat tissue wasting and hypoglycemia | J Clin Invest. 1993 Nov;92(5):2152-9. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00001230 | - | Recruiting | - | United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR) 800-441-1222 ext TTY8864111010 prpl@cc.nih.gov 收起 << | |
| NCT02347332 | Recurrent or Metastatic Head a... 展开 >>nd Neck Carcinoma 收起 << | Phase 3 | Active, not recruiting | June 2018 | - |
| NCT02871284 | Exercise Chem... 展开 >>otherapy-induced Polyneuropathy 收起 << | Phase 2 Phase 3 | Recruiting | December 2019 | Germany ... 展开 >> National Center for Tumor Diseases Recruiting Heidelberg, Germany, 69120 Contact: Joachim Wiskemann, Dr. joachim.wiskemann@nct-heidelberg.de Contact: Jana Müller jana.mueller@nct-heidelberg.de 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
0.70mL 0.14mL 0.07mL |
3.50mL 0.70mL 0.35mL |
7.00mL 1.40mL 0.70mL |
|
| CAS号 | 129-46-4 |
| 分子式 | C51H34N6Na6O23S6 |
| 分子量 | 1429.17 |
| SMILES Code | 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.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+] |
| MDL No. | MFCD00210217 |
| 别名 | 苏拉明钠盐 ;Suramin hexasodium salt; Suramin Sodium; NF 060; Germanin; BAY 205; Suramin (sodium salt) |
| 运输 | 蓝冰 |
| InChI Key | VAPNKLKDKUDFHK-UHFFFAOYSA-H |
| Pubchem ID | 8514 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 85 mg/mL(59.48 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 50 mg/mL(34.99 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的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
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