FMK

SKU: orb1678992

Description

This small molecule is a potent, irreversible inhibitor of the RSK2 (ribosomal S6 kinase 2) kinase. It is a valuable research tool for studying RSK2 signaling pathways in cellular and biochemical assays, with applications in cancer research and studies of cell proliferation.

Research Area

Signal Transduction

Key Properties

• CAS Number: 821794-92-7
• MW: 342.37
• Purity: 99.71% (May vary between batches)
• Formula: C₁₈H₁₉FN₄O₂
• SMILES: Cc1ccc(cc1)-c1c(C(=O)CF)n(CCCO)c2ncnc(N)c12
• Target: S6 Kinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (9.64 mM);H2O:Insoluble;DMSO:90 mg/mL (262.87 mM)

Bioactivity

• In Vitro:
  Pretreatment of ARVMs with 3 μM FMK mitigates the increase in Ser386 phosphorylation without affecting Thr577 phosphorylation . 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 . FMK deactivates the CTD auto-kinase activity of RSK1 and RSK2 with notable specificity in mammalian cells, reducing FGFR3-induced cytokine-independent growth in Ba/F3 cells and hindering cytokine-independent proliferation prompted by FGFR3 .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RSK2, S6Kinase, S6 Kinase, FMK

Compound Identifiers

PubChem CID

644243