Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FMK 是一种不可逆的 RSK2 抑制剂,能够共价修饰 RSK 的 C 末端区域。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 655 | 现货 | ||
2 mg | ¥ 957 | 现货 | ||
5 mg | ¥ 1,830 | 现货 | ||
10 mg | ¥ 2,770 | 现货 | ||
25 mg | ¥ 4,590 | 现货 | ||
50 mg | ¥ 6,580 | 现货 | ||
100 mg | ¥ 8,960 | 现货 | ||
500 mg | ¥ 17,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,880 | 现货 |
产品描述 | FMK is an irreversible inhibitor of RSK2 kinase. |
体外活性 | The pretreatment of ARVMs with 3 μM FMK attenuates the increase in Ser386 phosphorylation, but it has no inhibitory effect on the increase in Thr577 phosphorylation [1]. FMK inhibits relatively few protein kinases in the panel, although it does inhibit protein tyrosine kinases, such as Src, Lck, Yes and Eph-A2, as well as S6K1. FMK will not inhibit RSK if the N-terminal kinase domain is activated by a mechanism that is independent of the C-terminal domain[2]. Fmk potently inactivates the CTD auto-kinase activity of RSK1 and RSK2 with high specificity in mammalian cells. Targeting RSK2 by FMK attenuates FGFR3-induced cytokine-independent growth in Ba/F3 cells. FMK inhibits cytokine-independent proliferation of Ba/F3 cells conferred by FGFR3 [3]. |
激酶实验 | To determine the ability of FGFR3 to phosphorylate RSK2, 500 ng of purified recombinant RSK2 variants are incubated with 500 ng of recombinant active FGFR3 in 10 mM HEPES (pH 7.5), 150 mM NaCl, 1 mM DTT, 0.01% Triton-X-100, 10 mM MnCl2, and 200 μM ATP for 30 min at 30°C. Phosphorylation of Y529 RSK2 is detected by specific phospho-antibody. To determine kinase activity of RSK2 CTD variants, purified recombinant RSK2 CTD proteins (500 nM) are incubated with 500 nM of active ERK in 20 mM HEPES [pH 8.0], 10 mM MgCl2, 2 mM tris-(2-carboxyethyl)-phosphine (TCEP), and 200 μM ATP for 1 hr at 30°C. Kinase reactions are initiated by the addition of 5 μCi of [γ-32P] ATP and 100 μM peptide substrate (CTD-tide), followed by incubation for 20 min at room temperature. Kinase activity is determined using the standard disk phospho-cellulose assay [3]. |
细胞实验 | RSK2 expressing Ba/F3 cell lines are generated by retroviral transduction as described by using Ba/F3 cells stably expressing FGFR3 TDII with pMSCV-puro plasmids encoding myc-tagged RSK2 variants, followed by antibiotic selection. For cell viability assays, 1×10^5 Ba/F3 cells stably expressing FGFR3 are cultured in 24-well plates with media containing increasing concentrations of FMK, acidic FGF (10 nM), and heparin (30 μg/mL) in the absence of IL-3. The relative cell viability at each experimental time point is determined by using the Celltiter96AQueous One solution proliferation kit [3]. |
分子量 | 342.37 |
分子式 | C18H19FN4O2 |
CAS No. | 821794-92-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 90 mg/mL (262.9 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9208 mL | 14.6041 mL | 29.2082 mL | 73.0204 mL |
5 mM | 0.5842 mL | 2.9208 mL | 5.8416 mL | 14.6041 mL | |
10 mM | 0.2921 mL | 1.4604 mL | 2.9208 mL | 7.302 mL | |
20 mM | 0.146 mL | 0.7302 mL | 1.4604 mL | 3.651 mL | |
50 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.4604 mL | |
100 mM | 0.0292 mL | 0.146 mL | 0.2921 mL | 0.7302 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。
FMK 821794-92-7 MAPK PI3K/Akt/mTOR signaling S6 Kinase Inhibitor inhibitor inhibit