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FMK
- RSK inhibitor Fmk
- Soluble in DMSO
- MF: C18H19FN4O2
- MW: 342.37
Description
FMK is a potent, highly specific and irreversible p90 ribosomal S6 kinase (RSK1/RSK2) inhibitor that binds the C-terminal kinase domain ATP-binding site and blocks RSK autophosphorylation at Ser386.
RSK kinases act downstream of ERK/MAPK signaling to regulate transcription, translation, cell survival and proliferation. FMK is useful for dissecting RSK-specific outputs and has been used to study apoptosis in FGFR3-expressing tumor models.
Key Features
- Irreversible RSK1/RSK2 inhibitor
- Targets the C-terminal kinase domain ATP-binding site
- Blocks RSK autophosphorylation at Ser386
- Induces apoptosis in FGFR3-expressing myeloma models
Applications
- RSK kinase pathway studies
- ERK/MAPK downstream signaling research
- FGFR3-driven myeloma cell assays
- Irreversible kinase inhibitor mechanism studies
Note: FMK (IC50 value 15 nM for RSK2 in vitro) is more potent than another CTKD RSK inhibitor SL-0101 (IC50 value 85 nM for RSK2). Mechanistically, FMK (Axon 1848) irreversibly binds to the C-terminal kinase domain (CTKD), whereas the RSK inhibitor BI-D1870 (Axon 1528) acts as a reversible inhibitor at the N-terminal kinase domain (NTKD).
More Information
| Parent CAS No. | 821794-92-7 |
|---|---|
| Chemical Name | 1-(4-amino-7-(3-hydroxypropyl)-5-p-tolyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)-2-fluoroethanone |
| SMILES | C1C=C(C)C=CC=1C1=C(C(=O)CF)N(CCCO)C2N=CN=C(N)C1=2 |
| MFCD | N.A. |
| InChi | 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) |
| InChiKey | IKLGYJACVCXYIL-UHFFFAOYSA-N |
| CID | 644243 |
| Short Description | RSK inhibitor |
References
- MS Cohen et al. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 2005, 308(5726),1318–1321.
- S Kang et al. p90 ribosomal S6 kinase 2 promotes invasion and metastasis of human head and neck squamous cell carcinoma cells. J. Clin. Invest. 2010, 120(4), 1165–1177.
- Doehn et al. RSK Is a Principal Effector of the RAS-ERK Pathway for Eliciting a Coordinate Promotile/Invasive Gene Program and Phenotype in Epithelial Cells. Mol. Cell, 2009, 35(4), 511–522.
- TL Nguyen. Targeting RSK: an overview of small molecule inhibitors. Anticancer Agents Med. Chem. 2008, 8(7), 710-716.
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