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Suramin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Suramin图片
CAS NO:145-63-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
苏拉明
产品介绍
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)

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.
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.
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.