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FMK

FMK

产品编号 TQ0310   CAS 821794-92-7

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。

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FMK Chemical Structure
FMK, CAS 821794-92-7
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
重组蛋白限时优惠
产品目录号及名称: FMK (TQ0310)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

DMSO: 90 mg/mL (262.9 mM), Sonification is recommended.

溶液配制表

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

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TargetMol Library Books参考文献

1. Cuello F, et al. Evidence for direct regulation of myocardial Na+/H+ exchanger isoform 1 phosphorylation and activity by 90-kDa ribosomal S6 kinase (RSK): effects of the novel and specific RSK inhibitor fmk on responses to alpha1-adrenergic stimulation. 2. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. 3. Kang S, et al. FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway. Cancer Cell. 2007 Sep;12(3):187-9.
LY-2584702 tosylate salt S6K-18 BRD7389 GSK269962A AD80 Gossypin Vistusertib Lenaldekar

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 已知活性化合物库 经典已知活性库 激酶抑制剂库 抗卵巢癌化合物库 抗癌化合物库 共价抑制剂库 抗肥胖化合物库

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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。

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技术支持

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。

Keywords

FMK 821794-92-7 MAPK PI3K/Akt/mTOR signaling S6 Kinase Inhibitor inhibitor inhibit

 

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