标签归档：suramin

Suramin sodium salt(Synonyms: 苏拉明钠; Suramin hexasodium salt)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Suramin sodium salt (Synonyms: 苏拉明钠; Suramin hexasodium salt) 纯度: ≥98.0%

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。

Suramin sodium salt(Synonyms: 苏拉明钠; Suramin hexasodium salt)

Suramin sodium salt Chemical Structure

CAS No. : 129-46-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
25 mg ￥3000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor[1]. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM)[2]. Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM)[3][4]. Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor[5]. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent[6][7][8].

IC50 & Target

SIRT1

297 nM (IC50)

SIRT2

1.15 μM (IC50)

SIRT5

22 μM (IC50)

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 IC50 values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively[7].
Suramin blocks viral replication in Vero E6 cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

1429.17

Formula

C51H34N6Na6O23S6
CAS 号

129-46-4
中文名称

苏拉明钠
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 : ≥ 200 mg/mL (139.94 mM)

DMSO : 125 mg/mL (87.46 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Zhang YL, et al. Suramin is an active site-directed, reversible, and tight-binding inhibitor of protein-tyrosine phosphatases. J Biol Chem. 1998 May 15;273(20):12281-7.

    [2]. Trapp J, et al. Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins). ChemMedChem. 2007 Oct;2(10):1419-31.

    [3]. Schuetz A, et al. Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin. Structure. 2007 Mar;15(3):377-89.

    [4]. De Clercq E, et al. Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses. Cancer Lett. 1979 Nov;8(1):9-22.

    [5]. Wanchao Yin, et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat Struct Mol Biol. 2021 Mar;28(3):319-325.

    [6]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.

    [7]. Novaes RD, et al. Purinergic Antagonist Suramin Aggravates Myocarditis and Increases Mortality by EnhancingParasitism, Inflammation, and Reactive Tissue Damage in Trypanosoma cruzi-Infected Mice. Oxid Med Cell Longev. 2018 Sep 30;2018:7385639.

    [8]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.

    [9]. Xiaozhe Zhang, et al. Suramin and NF449 Are IP5K Inhibitors That Disrupt IP6-mediated Regulation of Cullin RING Ligase and Sensitize Cancer Cells to MLN4924/pevonedistat. J Biol Chem. 2020 Jun 3;jbc.RA120.014375.

    [10]. Xiaozhe Zhang, et al. Suramin and NF449 Are IP5K Inhibitors That Disrupt IP6-mediated Regulation of Cullin RING Ligase and Sensitize Cancer Cells to MLN4924/pevonedistat. J Biol Chem. 2020 Jun 3;jbc.RA120.014375.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Suramin(Synonyms: 苏拉明)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Suramin (Synonyms: 苏拉明)

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。

Suramin(Synonyms: 苏拉明)

Suramin Chemical Structure

CAS No. : 145-63-1

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Suramin 的其他形式现货产品:

Suramin sodium salt

生物活性

Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor[1]. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM)[2]. Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM)[3][4]. Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor[5].Suramin efficiently inhibits IP5K and is an antiparasitic, 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)

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 IC50 values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively[7].
Suramin blocks viral replication in Vero E6 cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

1297.28

Formula

C51H40N6O23S6
CAS 号

145-63-1
中文名称

苏拉明
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.
参考文献

  • [1]. Zhang YL, et al. Suramin is an active site-directed, reversible, and tight-binding inhibitor of protein-tyrosine phosphatases. J Biol Chem. 1998 May 15;273(20):12281-7.

    [2]. Trapp J, et al. Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins). ChemMedChem. 2007 Oct;2(10):1419-31.

    [3]. Schuetz A, et al. Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin. Structure. 2007 Mar;15(3):377-89.

    [4]. De Clercq E, et al. Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses. Cancer Lett. 1979 Nov;8(1):9-22.

    [5]. Wanchao Yin, et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat Struct Mol Biol. 2021 Mar;28(3):319-325.

    [6]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.

    [7]. Novaes RD, et al. Purinergic Antagonist Suramin Aggravates Myocarditis and Increases Mortality by EnhancingParasitism, Inflammation, and Reactive Tissue Damage in Trypanosoma cruzi-Infected Mice. Oxid Med Cell Longev. 2018 Sep 30;2018:7385639.

    [8]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.

    [9]. Xiaozhe Zhang, et al. Suramin and NF449 Are IP5K Inhibitors That Disrupt IP6-mediated Regulation of Cullin RING Ligase and Sensitize Cancer Cells to MLN4924/pevonedistat. J Biol Chem. 2020 Jun 3;jbc.RA120.014375.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务