FMK, inhibitor

FMK

Cat. Num. AAA5764557

• Purity: 98.00%
• Synonyms: FMK; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (292.08mM) Need ultrasonic; Water: Insoluble; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C18H19FN4O2
• SMILES: Cc(cc1)ccc1-c1c(C(CF)=O)n(CCCO)c2c1c(N)ncn2
• CAS Number: 821794-92-7
• 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, 1x10^5 Ba/F3 cells stably expressing FGFR3 are cultured in 24-well plates with media containing increasing concentrations of FMK, acidic FGF (10nM), and heparin (30ug/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].
• 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 10mM HEPES (pH 7.5), 150mM NaCl, 1mM DTT, 0.01% Triton-X-100, 10mM MnCl2, and 200uM ATP for 30 minutes at 30 degree C. Phosphorylation of Y529 RSK2 is detected by specific phospho-antibody. To determine kinase activity of RSK2 CTD variants, purified recombinant RSK2 CTD proteins (500nM) are incubated with 500nM of active ERK in 20mM HEPES [pH 8.0], 10mM MgCl2, 2mM tris-(2-carboxyethyl)-phosphine (TCEP), and 200uM ATP for 1 hr at 30 degree C. Kinase reactions are initiated by the addition of 5uCi of [gamma-32P] ATP and 100uM peptide substrate (CTD-tide), followed by incubation for 20 minutes at room temperature. Kinase activity is determined using the standard disk phospho-cellulose assay [3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for FMK, inhibitor

FMK is an irreversible inhibitor of RSK2 kinase.

Product Categories/Family for FMK, inhibitor

PI3K/Akt/mTOR signaling; S6 Kinase

References

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.
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.
Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
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.
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.