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Description: MSK/RSK family kinase inhibitor
Chemical Name: 2-Cyano-N-(2-hydroxy-1,1-dimethylethyl)-3-[3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl]-2-propenamide
Purity: ≥98% (HPLC)
Biological Activity
MSK/RSK family kinase inhibitor. Exhibits selectivity for RSK2 over NEK2 and PLK1 (IC50s are 12, 530 and 2200 nM, respectively). Inhibits MSK1, MSK2, RSK2 and RSK3 in cellular assays. Reduces CREB phosphorylation in HeLa cells.
Technical Data
| M. Wt | 450.5 |
| Formula | C24H26N4O5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1307896-46-3 |
| PubChem ID | 67206797 |
| InChI Key | FCCMYBKAZCDQGX-LZYBPNLTSA-N |
| Smiles | [H]/C(C1=CC=C(NN=C2C3=CC(OC)=C(OC)C(OC)=C3)C2=C1)=C(C#N)\C(NC(C)(C)CO)=O |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 450.5. 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 | 2.22 mL | 11.1 mL | 22.2 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Miller et al (2013) Electrophilic fragment-based design of reversible covalent kinase inhibitors. J.Am.Chem.Soc. 135 5298 PMID: 23540679
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Keywords: RMM 46, RMM 46 supplier, RMM46, RSK2, 3, MSK1, inhibitors, inhibits, family, kinases, CREB, phosphorylation, RSK, 5909, Tocris Bioscience
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Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases