2. MAPK/ERK Pathway
  3. Ribosomal S6 Kinase (RSK)
  4. FMK

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 Chemical Structure

CAS No. : 821794-92-7

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规格 价格 是否有货 数量
1 mg ￥679
In-stock
2 mg ￥960
In-stock
5 mg ￥1850
In-stock
10 mg ￥2800
In-stock
25 mg ￥4700
In-stock
50 mg 现货 询价
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of FMK:

FMK 相关抗体

Top Publications Citing Use of Products

查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

查看所有亚型
p70S6K RSK1 RSK2 RSK3 RSK4

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
COS-7 EC50
200 nM
Compound: fmk
Inhibition of EGF-stimulated RSK2 Ser386 autophosphorylation in serum starved african green monkey COS7 cells by immunoprecipitation and Western blot
Inhibition of EGF-stimulated RSK2 Ser386 autophosphorylation in serum starved african green monkey COS7 cells by immunoprecipitation and Western blot
[PMID: 15919995]
HEK293 EC50
150 nM
Compound: 1, fmk
Inhibition of PMA-stimulated RSK2 phosphorylation in HEK293 cells after 1 hr by Western blotting analysis
Inhibition of PMA-stimulated RSK2 phosphorylation in HEK293 cells after 1 hr by Western blotting analysis
[PMID: 17259979]
HeLa IC50
39 μM
Compound: 5; fmk
Inhibition of proteasomal turnover of p97-independent ODD-luciferase reporter substrate in human HeLa cells incubated for 120 mins by luciferase reporter gene assay
Inhibition of proteasomal turnover of p97-independent ODD-luciferase reporter substrate in human HeLa cells incubated for 120 mins by luciferase reporter gene assay
[PMID: 33476933]
体外研究
(In Vitro)

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 are 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 a specific small molecule RSK inhibitor fmk attenuates FGFR3-induced cytokine-independent growth in Ba/F3 cells. FMK inhibits cytokine-independent proliferation of Ba/F3 cells conferred by FGFR3[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FMK 相关抗体:
分子量

342.37

Formula

C18H19FN4O2
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (146.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9208 mL 14.6041 mL 29.2082 mL
5 mM 0.5842 mL 2.9208 mL 5.8416 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.30 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.30 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.45%

COA (270 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[3]

The S6 peptide kinase assay is carried out according to the manufacturer’s protocol using RSK2 immunoprecipitates. 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% Trixton-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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[3]

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, 1×105 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

FMK 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 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 7.3020 mL
15 mM 0.1947 mL 0.9736 mL 1.9472 mL 4.8680 mL
20 mM 0.1460 mL 0.7302 mL 1.4604 mL 3.6510 mL
25 mM 0.1168 mL 0.5842 mL 1.1683 mL 2.9208 mL
30 mM 0.0974 mL 0.4868 mL 0.9736 mL 2.4340 mL
40 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8255 mL
50 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4604 mL
60 mM 0.0487 mL 0.2434 mL 0.4868 mL 1.2170 mL
80 mM 0.0365 mL 0.1826 mL 0.3651 mL 0.9128 mL
100 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FMK821794-92-7Ribosomal S6 Kinase (RSK)S6KInhibitorinhibitorinhibit

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