An inhibitor of RSK2
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FMK

Item No. 9000887

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoro-ethanone
CAS Number
821794-92-7
Synonyms
  • Fluoromethyl Ketone
  • Fluoromethyl Ketone-MEA
  • FMK-MEA
Molecular Formula
C18H19FN4O2
Formula Weight
342.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
233, 331 nm
SMILES
FCC(C1=C(C2=CC=C(C)C=C2)C(C(N)=NC=N3)=C3N1CCCO)=O
InChi Code
InChI=1S/C18H19FN4O2/c1-11-3-5-12(6-4-11)14-15-17(20)21-10-22-18(15)23(7-2-8-24)16(14)13(25)9-19/h3-6,10,24H,2,7-9H2,1H3,(H2,20,21,22)
InChi Key
IKLGYJACVCXYIL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    Product Description

    FMK is an inhibitor of p90 ribosomal S6 kinase 3α (RSK2; IC50 = 15 nM).1 It inhibits the C-terminal domain (CTD) kinase activity of RSK2 and inhibits EGF-induced phosphorylation of RSK2 Ser386 in serum-starved COS-7 cells (EC50 = ~200 nM). FMK (6 µM) reduces invasion, but not proliferation, of M4e, 212LN, and 37B human head and neck squamous cell carcinoma cells.2 It also inhibits FGFR3-induced growth of Ba/F3 cells in a concentration-dependent manner and induces apoptosis in OPM-1, LP-1, and KMS-18 human myeloma cells expressing the t(4;14) translocation mutation and FGFR3 when used at a concentration of 10 µM.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cohen, M.S., Zhang, C., Shokat, K.M., et al. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 308(5726), 1318-1321 (2005).

    2. Kang, S., Elf, S., Lythgoe, K., et al. p90 ribosomal S6 kinase 2 promotes invasion and metastasis of human head and neck squamous cell carcinoma cells. J. Clin. Invest. 120(4), 1165-1177 (2010).

    3. Kang, S., Dong, S., Gu, T.-L., et al. FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway. Cancer Cell 12(3), 201-214 (2007).