676596-65-9
1-AZAKENPAULLONE
CAS: 676596-65-9
Molecular Formula: C15H10BrN3O
676596-65-9 - Names and Identifiers
| Name | 1-AZAKENPAULLONE |
| Synonyms | azakenpaullone 1-AZAKENPAULLONE InSolution? 1-Azakenpaullone |
| CAS | 676596-65-9 |
| EINECS | 200-258-5 |
676596-65-9 - Physico-chemical Properties
| Molecular Formula | C15H10BrN3O |
| Molar Mass | 328.16 |
| Density | 1.655±0.06 g/cm3(Predicted) |
| Melting Point | >290°C (dec.) |
| Boling Point | 648.8±50.0 °C(Predicted) |
| Solubility | DMSO: >10mg/mL |
| Appearance | Tan solid |
| Color | gray-brown |
| pKa | 13.36±0.20(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 1-azakenpaulone selectively inhibited CDK1/cyclin B, CDK5/p25 and GSK-3β activity with IC50 values of 0.018 μm, 4.2 μm and 2.0 μm, respectively. In human islet cells, the combination of 1-azakenpaulone (5 mM) and glucose (8 mM) inhibited β-cell proliferation. 1-azakenpaulone effectively induced INS-1E of cells to replicate and protected INS-1E of cells from cell death caused by liposidic toxicity. |
| In vivo study | 1-azakenpaulone (10 or 100 pmol, intracerebral injection) pretreatment attenuates ketamine-induced hyperkinesia, PPI disruption, cognitive deficits, and in the rotation test to raise the ketamine caused by the movement of uncoordinated. |
676596-65-9 - Risk and Safety
| WGK Germany | 2 |
676596-65-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.047 ml | 15.236 ml | 30.473 ml |
| 5 mM | 0.609 ml | 3.047 ml | 6.095 ml |
| 10 mM | 0.305 ml | 1.524 ml | 3.047 ml |
| 5 mM | 0.061 ml | 0.305 ml | 0.609 ml |
Last Update：2024-01-02 23:10:35
676596-65-9 - Reference Information
| biological activity | 1-Azakenpaullone (1-Akp) is a highly selective GSK-3β inhibitor with IC50 of 18 nM, and its selectivity is 100 times higher than CDK1/cyclin B and CDK5/p25. |
| target | TargetValue GSK-3α GSK-3β (Cell-free say) 18 nM |
| Target | Value |
| GSK-3α | |
| GSK-3β (Cell-free assay) | 18 nM |
| in vitro study | 1-Azakenpaullone can selectively inhibit CDK1/cyclin B, CDK5/p25 and GSK-3β activities with IC50 values of 0.018 μM, 4.2 μM and 2.0 μM respectively. In human islet cells, the combination of 1-Azakenpaullone (5 mM) and glucose (8 mM) inhibited the proliferation of β cells. 1-Azakenpaullone was effective in inducing INS-1E cell replication and protecting INS-1E cells from cell death induced by lipotoxicity. |
| in vivo study | 1-Azakenpaullone (10 or 100 pmol, intracerebral injection) pretreatment can weaken hyperkinesia, PPI interruption and cognitive deficiency caused by catamentin, and improve the incoordination caused by catamentin in rotation test. |
Last Update：2024-04-09 20:52:54
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