Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LJH685 是一种选择性,ATP-竞争性的RSK 抑制剂, 抑制 RSK1/2/3 生物活性,IC50为 6、5、4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 316 | 现货 | ||
2 mg | ¥ 459 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,650 | 现货 | ||
50 mg | ¥ 3,960 | 现货 | ||
100 mg | ¥ 5,650 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 867 | 现货 |
产品描述 | LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM). |
靶点活性 | RSK1:6 nM, RSK2:5 nM, RSK3:4 nM |
体外活性 | LJH685 modulates YB1 phosphorylation by potently and selectively inhibiting RSK in cells. In MAPK pathway–dependent cancer cell lines, LJH685 shows antiproliferative effects, and causes cell-cycle regulation and apoptosis induction. [1] |
激酶实验 | Inhibition of RSK1, RSK2, and RSK3 activity: Enzymatic activity of RSK isoforms 1, 2, and 3 (PV4049, PV4051, and PV3846) is assessed using recombinant full-length RSK protein. RSK1 (1 nmol/L), RSK2 (0.1 nmol/L), or RSK3 (1 nmol/L) is allowed to phosphorylate 200 nmol/L peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1, 5 μmol/L; RSK2, 20 μmol/L; and RSK3, 10 μmol/L) and appropriate dilutions of RSK inhibitors. |
细胞实验 | Cell growth under attached conditions is assessed by plating 1000 cells per well on 96-well tissue culture-treated plates in cell growth medium. Appropriate dilutions of compound are added medium above cells and cell growth is assessed after 72 hrs by addition of CellTiter Glo reagent according to manufacturer's directions.(Only for Reference) |
分子量 | 381.42 |
分子式 | C22H21F2N3O |
CAS No. | 1627710-50-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 71 mg/mL (186.1 mM)
Ethanol: 16 mg/mL (41.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL | 65.5445 mL |
5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | 13.1089 mL | |
10 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL | 6.5545 mL | |
20 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2772 mL | |
DMSO | 50 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3109 mL |
100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6554 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。
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