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

FMK 

Cat. No.: HY-52101A Purity: 99.30%
Handling Instructions

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

For research use only. We do not sell to patients.

FMK Chemical Structure

FMK Chemical Structure

CAS No. : 821794-92-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 249 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 384 In-stock
Estimated Time of Arrival: December 31
25 mg USD 768 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of FMK:

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Description

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

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].

Molecular Weight

342.37

Formula

C₁₈H₁₉FN₄O₂

CAS No.

821794-92-7

SMILES

FCC(C1=C(C2=C(N=CN=C2N1CCCO)N)C3=CC=C(C=C3)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (292.08 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2921 mL 1.4604 mL 2.9208 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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.

References

Purity: 99.30%

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Keywords:

FMKRibosomal S6 Kinase (RSK)S6KInhibitorinhibitorinhibit

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