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Description: Potent and selective GSK3 inhibitor. Used in chemical cocktail for induction and maintainance of TotiSCs.
Alternative Names: 1-Akp
Chemical Name: 9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one
Purity: ≥98% (HPLC)
Biological Activity for 1-Azakenpaullone
1-Azakenpaullone is a potent and selective inhibitor of glycogen synthase kinase 3 (GSK-3), with IC50 = 18 nM. It displays selectivity index (SI) of 111 and 233 over CDK1 and CDK5, respectively.
1-Azakenpaullone stimulates growth and replication of β-cells in vitro (rat islets) and alleviates glucolipotoxicity in INS-1 β-cells. It displays mitogenic effects on rat β-cells comparable with those of incretin hormone GIP.
In combination with TTNPB (Cat. No. 0761) and WS 6 (Cat. No. 7791), 1-Azakenpaullone can be part of a chemical cocktail used for induction and long-term maintainance in vitro of totipotent stem cells (TotiSCs) from mouse pluripotent stem cells (PSCs).
Technical Data for 1-Azakenpaullone
| M. Wt | 328.17 |
| Formula | C15H10BrN3O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 676596-65-9 |
| PubChem ID | 6538897 |
| InChI Key | NTSBZVCEIVPKBJ-UHFFFAOYSA-N |
| Smiles | BrC2=CC=C1NC3=C(CC(NC4=C3N=CC=C4)=O)C1=C2 |
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 for 1-Azakenpaullone
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.82 | 100 |
Preparing Stock Solutions for 1-Azakenpaullone
The following data is based on the product molecular weight 328.17. 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 | 3.05 mL | 15.24 mL | 30.47 mL |
| 5 mM | 0.61 mL | 3.05 mL | 6.09 mL |
| 10 mM | 0.3 mL | 1.52 mL | 3.05 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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Product Datasheets for 1-Azakenpaullone
References for 1-Azakenpaullone
References are publications that support the biological activity of the product.
Kunick et al (2004) 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β. Bioorg.Med.Chem.Lett. 14 413 PMID: 14698171
Mussmann et al (2007) Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. J.Biol.Chem. 282 12030 PMID: 17242403
Hu et al (2023) Induction of mouse totipotent stem cells by a defined chemical cocktail. Nature 617 792 PMID: 35728625
If you know of a relevant reference for 1-Azakenpaullone, please let us know.
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Pathways for 1-Azakenpaullone
