FMK
Based on 4 publication(s) in Google Scholar
FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
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- 純度: 99.83%
- CAS 番号: 821794-92-7
- 分子式: C18H19FN4O2
- 分子量:342.37
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 FMK
More
生物活性
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RSK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
200 nM
Compound: fmk
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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
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[PMID: 15919995] |
| HEK293 | EC50 |
150 nM
Compound: 1, fmk
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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
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[PMID: 17259979] |
| HEK293 | IC50 |
15 nM
Compound: 5, FMK
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Inhibition of RSK2 transfected in HEK293 cells
Inhibition of RSK2 transfected in HEK293 cells
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[PMID: 22621397] |
| HeLa | IC50 |
39 μM
Compound: 5; fmk
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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
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[PMID: 33476933] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 821794-92-7
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性状 Solid
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分子量 342.37
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分子式 C18H19FN4O2
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Color White to light yellow
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SMILES
FCC(C1=C(C2=C(N=CN=C2N1CCCO)N)C3=CC=C(C=C3)C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (4)
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Journal Impact Factor
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Most Recent
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Mol Cell
2020 Oct 15;80(2):296-310.e6. PMID: 32979304 -
J Extracell Vesicles
ADAM Sheddase Activity Promotes the Detachment of Small Extracellular Vesicles From the Plasma Membrane. [Abstract]2025 Jul;14(7):e70114. PMID: 40673783 -
Cell Rep
EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer. [Abstract]2022 Dec 13;41(11):111827. PMID: 36516759 -
Cancers
FLT3-ITD Activates RSK1 to Enhance Proliferation and Survival of AML Cells by Activating mTORC1 and eIF4B Cooperatively with PIM or PI3K and by Inhibiting Bad and BIM. [Abstract]2019 Nov 20;11(12):1827. PMID: 31756944
溶剤 & 溶解度
DMSO : 50 mg/mL (146.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |
FMK 関連分類
HY-52101A 関連分類
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