SURAMIN
- CAS号:145-63-1
- 英文名:8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bisnaphthalene-1,3,5-trisulphonic acid
- 中文名:SURAMIN
- CBNumber:CB8906847
- 分子式:C51H40N6O23S6
- 分子量:1297.28
- MOL File:145-63-1.mol
- 熔点 :128 °C(Solv: ethyl ether (60-29-7))
- 密度 :1.2629 (rough estimate)
- 折射率 :1.7770 (estimate)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :-1.35±0.40(Predicted)
- 颜色 :Pinkish-white, hygroscopic powder
- EPA化学物质信息 :Suramin (145-63-1)
- 毒性 :LD50 intravenous in mouse: 620mg/kg
SURAMIN性质、用途与生产工艺
- 生物活性 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。
-
靶点
SIRT1
297 nM (IC 50 )
SIRT2
1.15 μM (IC 50 )
SIRT5
22 μM (IC 50 )
-
体外研究
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.
Suramin (300 μg/mL; for 48 hours) induces cells apoptosis, and down-regulates mRNA expression in HeLa cells.
Suramin (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2.
The IC 50 values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively.
Suramin blocks viral replication in Vero E6 cells.
Cell Proliferation Assay
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
Cell Line: HeLa cells Concentration: 300 μg/mL Incubation Time: For 48 hours Result: Induced cells apoptosis. Western Blot Analysis
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
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.
Animal Model: Adult male Wistar rats (200-225 g) 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. - 类别 有毒物品
- 毒性分级 中毒
- 急性毒性 静脉-小鼠 LD50: 620 毫克/公斤
- 可燃性危险特性 可燃; 燃烧产生有毒氮氧化物和硫氧化物烟雾
- 储运特性 通风低温干燥
- 灭火剂 干粉,泡沫,沙土,二氧化碳, 雾状水
- 公司名称：Service Chemical Inc.
- 联系电话：--
- 电子邮件：sales@chemos-group.com
- 国家：德国
- 产品数：6350
- 优势度：71
