Synonyms: azakenpaullone
Compound class:
Synthetic organic
Comment: 1-azakenpaullone is a potent and selective ATP-competitive inhibitor of glycogen synthase kinase-3β (GSK-3β) [4]. In contrast to other paullones, this analogue has insignificant activity at the phylogenetically related cyclin-dependent kinases (CDKs) CDK1 and CDK5. 1-azakenpaullone is compound 16 in [4].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Cai Z, Zhao Y, Zhao B. (2012)
Roles of glycogen synthase kinase 3 in Alzheimer's disease. Curr Alzheimer Res, 9 (7): 864-79. [PMID:22272620] |
2. Eldar-Finkelman H, Schreyer SA, Shinohara MM, LeBoeuf RC, Krebs EG. (1999)
Increased glycogen synthase kinase-3 activity in diabetes- and obesity-prone C57BL/6J mice. Diabetes, 48 (8): 1662-6. [PMID:10426388] |
3. Hurtado DE, Molina-Porcel L, Carroll JC, Macdonald C, Aboagye AK, Trojanowski JQ, Lee VM. (2012)
Selectively silencing GSK-3 isoforms reduces plaques and tangles in mouse models of Alzheimer's disease. J Neurosci, 32 (21): 7392-402. [PMID:22623685] |
4. Kunick C, Lauenroth K, Leost M, Meijer L, Lemcke T. (2004)
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett, 14 (2): 413-6. [PMID:14698171] |
5. Nikoulina SE, Ciaraldi TP, Mudaliar S, Mohideen P, Carter L, Henry RR. (2000)
Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes. Diabetes, 49 (2): 263-71. [PMID:10868943] |
6. Takashima A, Noguchi K, Sato K, Hoshino T, Imahori K. (1993)
Tau protein kinase I is essential for amyloid beta-protein-induced neurotoxicity. Proc Natl Acad Sci USA, 90 (16): 7789-93. [PMID:8356085] |