Biological Activity
Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 31 nM for GSK-3α); competes with ATP. Has minimal activity against 24 other protein kinases (IC50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 359.73 |
| Formula | C16H10ClN3O5 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 264218-23-7 |
| PubChem ID | 4210951 |
| InChI Key | PQCXVIPXISBFPN-UHFFFAOYSA-N |
| Smiles | OC1=C(Cl)C=C(NC2=C(C(=O)NC2=O)C2=C(C=CC=C2)[N+]([O-])=O)C=C1 |
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 | 17.99 | 50 | |
| ethanol | 8.99 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 359.73. 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 | 2.78 mL | 13.9 mL | 27.8 mL |
| 5 mM | 0.56 mL | 2.78 mL | 5.56 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Coghlan et al (2000) Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem.Biol. 7 793 PMID: 11033082
Cross et al (2001) Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J.Neurochem. 77 94 PMID: 11279265
Liang and Chuang (2006) Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J.Biol.Chem. 282 3904 PMID: 17148450
Keywords: SB 415286, supplier, Potent, selective, GSK-3, inhibitors, inhibits, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB415286, GlaxoSmithKline, GSK, Glycogen, Synthase, Kinase, 3, Glycogen, Synthase, Kinase, Glycogen, Synthase, Kinase, 3, Tocris Bioscience
