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FMK

FMK
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Purity:98.93%
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FMK

Catalog No. TQ0310Cas No. 821794-92-7
FMK is an irreversible inhibitor of RSK2 kinase.
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
Pack SizePriceAvailabilityQuantity
1 mg$68In Stock
2 mg$97In Stock
5 mg$177In Stock
10 mg$317In Stock
25 mg$538In Stock
50 mg$777In Stock
100 mg$1,090In Stock
500 mg$2,170In Stock
1 mL x 10 mM (in DMSO)$197In Stock
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Product Introduction

Bioactivity
Description
FMK is an irreversible inhibitor of RSK2 kinase.
In vitro
Pretreatment of ARVMs with 3 μM FMK mitigates the increase in Ser386 phosphorylation without affecting Thr577 phosphorylation [1]. FMK selectively inhibits a limited range of protein kinases, notably including protein tyrosine kinases such as Src, Lck, Yes, and Eph-A2, alongside S6K1. It does not inhibit RSK when the N-terminal kinase domain is activated independently of the C-terminal domain [2]. Moreover, FMK effectively deactivates the CTD auto-kinase activity of RSK1 and RSK2 with notable specificity in mammalian cells. By targeting RSK2, FMK reduces FGFR3-induced cytokine-independent growth in Ba/F3 cells and hinders the cytokine-independent proliferation prompted by FGFR3 in the same cells [3].
Kinase Assay
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].
Cell Research
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].
Chemical Properties
Molecular Weight342.37
FormulaC18H19FN4O2
Cas No.821794-92-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: Insoluble
DMSO: 90 mg/mL (262.9 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9208 mL14.6041 mL29.2082 mL146.0408 mL
5 mM0.5842 mL2.9208 mL5.8416 mL29.2082 mL
10 mM0.2921 mL1.4604 mL2.9208 mL14.6041 mL
20 mM0.1460 mL0.7302 mL1.4604 mL7.3020 mL
50 mM0.0584 mL0.2921 mL0.5842 mL2.9208 mL
100 mM0.0292 mL0.1460 mL0.2921 mL1.4604 mL

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