Biological Activity
Potent, ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor (IC50 = 11 nM in an in vitro kinase assay); targets the N-terminal kinase domain. Inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells. Blocks IL-10 production in macrophages.
Licensing Information
Sold with the permission of GlaxoSmithKline.
Compound Libraries
SB 747651A dihydrochloride is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox II and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 415.32 |
| Formula | C16H22N8O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1781882-72-1 |
| PubChem ID | 90488958 |
| InChI Key | NRRCQHARLPNLHJ-UHFFFAOYSA-N |
| Smiles | NC1=NON=C1C3=NC2=CN=CC(CNC4CCNCC4)=C2N3CC.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.77 | 50 | |
| water | 20.77 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 415.32. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.41 mL | 12.04 mL | 24.08 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.82 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.41 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bamford et al (2005) (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors. Bioorg.Med.Chem.Lett. 15 3402 PMID: 15950465
Bamford et al (2005) (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors. Bioorg.Med.Chem.Lett. 15 3407 PMID: 15955699
Naqvi et al (2012) Characterization of the cellular action of the MSK inhibitor SB-747651A. Biochem.J. 441 347 PMID: 21970321
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