Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK591 (GSK3203591) 是一种有效的精氨酸甲基转移酶 PRMT5 选择性抑制剂,IC50值为 11 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 306 | 现货 | ||
2 mg | ¥ 466 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,580 | 现货 | ||
100 mg | ¥ 6,530 | 现货 | ||
500 mg | ¥ 13,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 983 | 现货 |
产品描述 | GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM). |
靶点活性 | PRMT5:11 nM |
体外活性 | In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases[1][2]. |
激酶实验 | Selectivity profiling experiments: The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or GSK2141795) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide. |
别名 | GSK3203591, EPZ015866 |
分子量 | 380.48 |
分子式 | C22H28N4O2 |
CAS No. | 1616391-87-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.3 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL | 65.7065 mL |
5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | 13.1413 mL | |
10 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL | 6.5706 mL | |
20 mM | 0.1314 mL | 0.6571 mL | 1.3141 mL | 3.2853 mL | |
50 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL | 1.3141 mL | |
100 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6571 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK591 1616391-87-7 Chromatin/Epigenetic Histone Methyltransferase EPZ 015866 GSK 591 EPZ-015866 Inhibitor inhibit GSK-3203591 GSK3203591 GSK 3203591 EPZ015866 GSK-591 inhibitor