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Description: Irreversible ribosomal S6 kinase 1/2 inhibitor
Chemical Name: 1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone
Purity: ≥97% (HPLC)
Biological Activity for Fmk
Fmk is a potent irreversible RSK1/2 inhibitor (IC50 = 15 nM). Inactivates the C-terminal auto-kinase domain activity. Suppresses RSK2 kinase activity in RSK2-expressing HNSCC cell lines. Reduces HNSCC cell invasive ability. Displays no effect on EGF-stimulated phosphorylation of ERK1 or ERK2.
Technical Data for Fmk
| M. Wt | 342.37 |
| Formula | C18H19FN4O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 821794-92-7 |
| PubChem ID | 644243 |
| InChI Key | IKLGYJACVCXYIL-UHFFFAOYSA-N |
| Smiles | O=C(CF)C2=C(C3=CC=C(C)C=C3)C1=C(N)N=CN=C1N2CCCO |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Fmk
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.24 | 100 |
Preparing Stock Solutions for Fmk
The following data is based on the product molecular weight 342.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.92 mL | 14.6 mL | 29.21 mL |
| 5 mM | 0.58 mL | 2.92 mL | 5.84 mL |
| 10 mM | 0.29 mL | 1.46 mL | 2.92 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets for Fmk
References for Fmk
References are publications that support the biological activity of the product.
Cohen et al (2005) Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 308 1318 PMID: 15919995
Cohen et al (2007) A clickable inhibitor reveals context-dependent autoactivation of p90 RSK. Nat.Chem.Biol. 3 156 PMID: 17259979
Kang et al (2010) p90 ribosomal S6 kinase 2 promotes invasion and metastasis of human head and neck squamous cell carcinoma cells. J.Clin.Invest. 120 1165 PMID: 20234090
If you know of a relevant reference for Fmk, please let us know.
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Keywords: Fmk, Fmk supplier, RSK-FMK, Irreversible, RSK1, RSK2, inhibitors, inhibits, p90, ribosomal, protein, S6, kinases, potent, RSK, 4690, Tocris Bioscience
Citations for Fmk
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Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
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- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases