中文名称: | AMI-1 disodium salt | ||||
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英文名称: | AMI-1 disodium salt | ||||
别名: | 猩红酸钠盐;6,6'-(1,3-亚脲基)双(1-萘酚-3-磺酸钠);猩红酸钠 AMI1;Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate) | ||||
CAS No: | 20324-87-2 | 分子式: | C21H14N2Na2O9S2 | 分子量: | 548.45 |
CAS No: | 20324-87-2 | ||||
分子式: | C21H14N2Na2O9S2 | ||||
分子量: | 548.45 | ||||
EINEC: | 243-735-4 | ||||
EINEC: | 243-735-4 |
基本信息
产品编号:A12005 |
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产品名称:AMI-1 disodium salt |
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CAS: |
20324-87-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量: |
548.45 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL warmed with 50ºC water bath (182.33mM) |
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Ethanol |
Insoluble |
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Water |
22mg/mL (40.11mM) |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.8233mL |
9.1166mL |
18.2332mL |
5mM |
0.3647mL |
1.8233mL |
3.6466mL |
10mM |
0.1823mL |
0.9117mL |
1.8233mL |
50mM |
0.0365mL |
0.1823mL |
0.3647mL |
生物活性
产品描述 |
一种有效的细胞渗透性的可逆的蛋白精氨酸 N-甲基转移酶(PRMTs)抑制剂。 |
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靶点/IC50 |
yeast Hmt1p |
human PRMT1 |
3.0μM |
8.8μM |
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体外研究 |
AMI-1 can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1,-3,-4,and -6 and Hmt1p).AMI-1 not only inhibits type I PRMTs (PRMT1,3,4 and 6) but also type II PRMT5.AMI-1 specifically inhibits arginine,but not lysine,methyltransferase activity in vitro and does not compete for the AdoMet binding site.AMI-1 inhibits methylation of GFP-Npl3 and cellular proteins.AMI-1 (0.6-2.4mM;48-96 hours) inhibits the cell viability of sarcoma in S180 and U2OS cells in a time-dependent and dosedependent manner in vitro.AMI-1 (1.2-2.4mM;48-72 hours) reduces S180 cell viability through the induction of cell apoptosis. |
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Cell Line: |
S180 cells,U2OS cells. |
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Concentration: |
0.6mM,1.2mM,2.4mM |
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Incubation Time: |
48 hours,72 hours,96 hours. |
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Result: |
Inhibited the cell viability. |
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Apoptosis Analysis |
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Cell Line: |
S180 cells. |
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Concentration: |
1.2mM,2.4mM |
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Incubation Time: |
48 hours,72 hours. |
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Result: |
Increased the percentages of cells undergoing apoptosis. |
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体内研究 |
AMI-1 (0.5mg;intratumorally;daily;for 7 days) inhibits S180 viability in vivo.AMI-1 (0.5mg;intratumorally;daily;for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model.AMI-1 (0.5mg;intratumorally;daily;for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model. |
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Animal Model: |
6-7 weeks old male Kunming mice (18-22g),with S180 cells xenograft. |
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Dosage: |
0.5mg |
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Administration: |
Intratumorally,daily,for 7 days. |
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Result: |
Decreased tumor weight. |
推荐实验方法(仅供参考)
激酶实验: |
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体外甲基化试验 |
所有甲基化反应在S-腺苷-L-[甲基-3H]蛋氨酸([3H]AdoMet,12.6μM 储备溶液在HCl/乙醇9:1中稀释得到79 Ci/mmol,pH 2.0–2.5)和PBS (137mM NaCl,2.7mM KCl,4.3mM Na2HPO4,1.4mM KH2PO4,pH 7.4)存在下进行。反应在5μg小分子抑制剂存在下于30-μL体积中进行,这意味着每个化合物的浓度如下:AMI-1,303μM;AMI-2,642μM;AMI-3, 690μM;AMI-4,520μM;AMI-5,257μM;AMI-6,336μM;AMI-7,265μM;AMI-8,247μM;AMI-9,325μM;AMA-1,439μM;AMA-2,503μM;和sinefungin,437μM。关于个别反应条件的其它信息在每个图例中阐明。样品在10% SDS-PAGE上分离,转移到PVDF膜,用Enhance™雾化,并曝光过夜。谱带强度使用Kodak 影像站440 和1D图像分析软件计算。 |
动物实验: |
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动物模型 |
慢性 AIPI 大鼠 |
剂量 |
50μL浓度为0.1mg/mL的溶液 |
给药处理 |
鼻内注射 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )