Biological Activity
Protein kinase inhibitor; inhibits cyclin-dependent kinases (IC50 = 0.18 - 3.33 μM) and GSK-3β (IC50 = 0.19 μM). Inhibits CDK5- and GSK-3β-mediated tau phosphorylation, a process over-active in Alzheimer disease states. Also inhibits AMPK, LCK and SGK. Induces cell cycle arrest and inhibits cell proliferation.
Technical Data
| M. Wt | 277.28 |
| Formula | C16H11N3O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 160807-49-8 |
| PubChem ID | 5326739 |
| InChI Key | LDEWQRSYYHTQRA-UHFFFAOYSA-N |
| Smiles | ON=C1C2=CC=CC=C2NC/1=C1C(=O)NC2=C1C=CC=C2 |
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 | 27.73 | 100 | |
| ethanol | 27.73 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 277.28. 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 | 3.61 mL | 18.03 mL | 36.06 mL |
| 5 mM | 0.72 mL | 3.61 mL | 7.21 mL |
| 10 mM | 0.36 mL | 1.8 mL | 3.61 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199 PMID: 12534346
Hoessel et al (1999) Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases. Nat.Cell.Biol. 1 60 PMID: 10559866
Leclerc et al (2001) Indirubins inhibit glycogen synthase kinase-3β and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. J.Biol.Chem. 276 251 PMID: 11013232
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