Date published: 2025-12-5

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1-Azakenpaullone (CAS 676596-65-9)

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Alternate Names:
9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one; 1-AKP; kenpaullone;
Application:
1-Azakenpaullone is a Kenpaullone analog and an inhibitor of GSK-3
CAS Number:
676596-65-9
Molecular Weight:
328.20
Molecular Formula:
C15H10BrN3O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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1-Azakenpaullone is a synthetic molecule classified as a paullone derivative, which is part of a broader category of compounds known as kenpaullones. These compounds are notable for their ability to inhibit cyclin-dependent kinases (CDKs), with a particular emphasis on CDK1, CDK2, CDK5, and glycogen synthase kinase 3 beta (GSK-3β). As an inhibitor, 1-Azakenpaullone exhibits strong selectivity and potency, making it a useful tool in the study of cell cycle regulation and neuronal signaling pathways. The mechanism of action of 1-Azakenpaullone involves the competitive inhibition of ATP binding sites on the target kinases. This inhibition alters the phosphorylation status of various substrates involved in critical signaling pathways that govern cellular processes such as cell division, differentiation, and apoptosis. Specifically, its inhibition of GSK-3β is of particular interest in research focused on neurodegenerative diseases and neural development, as GSK-3β is a key player in neuronal cell function and structure.


1-Azakenpaullone (CAS 676596-65-9) References

  1. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.  |  Kunick, C., et al. 2004. Bioorg Med Chem Lett. 14: 413-6. PMID: 14698171
  2. Planarian GSK3s are involved in neural regeneration.  |  Adell, T., et al. 2008. Dev Genes Evol. 218: 89-103. PMID: 18202849
  3. Inhibition of Gsk3β activity improves β-cell function in c-KitWv/+ male mice.  |  Feng, ZC., et al. 2012. Lab Invest. 92: 543-55. PMID: 22249311
  4. Inhibition of glycogen synthase kinase-3 attenuates psychotomimetic effects of ketamine.  |  Chan, MH., et al. 2012. Schizophr Res. 136: 96-103. PMID: 22325078
  5. Combination effects of AHR agonists and Wnt/β-catenin modulators in zebrafish embryos: Implications for physiological and toxicological AHR functions.  |  Wincent, E., et al. 2015. Toxicol Appl Pharmacol. 284: 163-79. PMID: 25711857
  6. WNT3 and membrane-associated β-catenin regulate trophectoderm lineage differentiation in human blastocysts.  |  Krivega, M., et al. 2015. Mol Hum Reprod. 21: 711-22. PMID: 26108805
  7. High-content screening assay-based discovery of paullones as novel podocyte-protective agents.  |  Lee, HW., et al. 2018. Am J Physiol Renal Physiol. 314: F280-F292. PMID: 29046299
  8. Insights into intestinal regeneration signaling mechanisms.  |  Bello, SA., et al. 2020. Dev Biol. 458: 12-31. PMID: 31605680
  9. Induction of mouse totipotent stem cells by a defined chemical cocktail.  |  Hu, Y., et al. 2023. Nature. 617: 792-797. PMID: 35728625
  10. Inhibition of GSK-3β Enhances Osteoblast Differentiation of Human Mesenchymal Stem Cells through Wnt Signalling Overexpressing Runx2.  |  AlMuraikhi, N., et al. 2023. Int J Mol Sci. 24: PMID: 37108323

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

1-Azakenpaullone, 1 mg

sc-358615
1 mg
$98.00