1-Azakenpaullone - CAS 676596-65-9
Catalog number: 676596-65-9
Category: Inhibitor
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1-Azakenpaullone inhibits glycogen synthase kinase 3β (GSK3β) more potently (IC50 = 18 nM) than CDK1/cyclin B or CDK5/p25 (IC50s = 2.0 and 4.2 µM, respectively).
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1.Polycyclic aromatic hydrocarbons and dibutyl phthalate disrupt dorsal-ventral axis determination via the Wnt/β-catenin signaling pathway in zebrafish embryos.
Fairbairn EA;Bonthius J;Cherr GN Aquat Toxicol. 2012 Nov 15;124-125:188-96. doi: 10.1016/j.aquatox.2012.08.017. Epub 2012 Aug 28.
The canonical Wnt/β-catenin signaling pathway is critical during early teleost development for establishing the dorsal-ventral axis. Within this pathway, GSK-3β, a key regulatory kinase in the Wnt pathway, regulates β-catenin degradation and thus the ability of β-catenin to enter nuclei, where it can activate expression of genes that have been linked to the specification of the dorsal-ventral axis. In this study, we describe the morphological abnormalities that resulted in zebrafish embryos when axis determination was disrupted by environmental contaminants. These abnormalities were linked to abnormal nuclear accumulation of β-catenin. Furthermore, we demonstrated that the developmental abnormalities and altered nuclear β-catenin accumulation occurred when embryos were exposed to commercial GSK-3β inhibitors. Zebrafish embryos were exposed to commercially available GSK-3 inhibitors (GSK-3 Inhibitor IX and 1-azakenpaullone), or common environmental contaminants (dibutyl phthalate or the polycyclic aromatic hydrocarbons phenanthrene and fluorene) from the 2 to 8-cell stage through the mid-blastula transition (MBT). These embryos displayed morphological abnormalities at 12.5 h post-fertilization (hpf) that were comparable to embryos exposed to lithium chloride (LiCl) (300 mM LiCl for 10 min, prior to the MBT), a classic disruptor of embryonic axis determination.
2.Glycogen synthase kinases 3alpha and 3beta in cardiac myocytes: regulation and consequences of their inhibition.
Markou T;Cullingford TE;Giraldo A;Weiss SC;Alsafi A;Fuller SJ;Clerk A;Sugden PH Cell Signal. 2008 Jan;20(1):206-18. Epub 2007 Oct 12.
Inhibition of glycogen synthase kinase 3beta (GSK3beta) as a consequence of its phosphorylation by protein kinase B/Akt (PKB/Akt) has been implicated in cardiac myocyte hypertrophy in response to endothelin-1 or phenylephrine. We examined the regulation of GSK3alpha (which we show to constitute a significant proportion of the myocyte GSK3 pool) and GSK3beta in cardiac myocytes. Although endothelin increases phosphorylation of GSK3 and decreases its activity, the response is less than that induced by insulin (which does not promote cardiac myocyte hypertrophy). GSK3 phosphorylation induced by endothelin requires signalling through the extracellular signal-regulated kinase 1/2 (ERK1/2) cascade and not the PKB/Akt pathway, whereas the reverse is true for insulin. Cardiac myocyte hypertrophy involves changes in morphology, and in gene and protein expression. The potent GSK3 inhibitor 1-azakenpaullone increases myocyte area as a consequence of increased cell length whereas phenylephrine increases both length and width. Azakenpaullone or insulin promotes AP1 transcription factor binding to an AP1 consensus oligonucleotide, but this was significantly less than that induced by endothelin and derived principally from increased binding of JunB protein, the expression of which was increased.
3.Ectopic activation of the canonical wnt signaling pathway affects ectodermal patterning along the primary axis during larval development in the anthozoan Nematostella vectensis.
Marlow H;Matus DQ;Martindale MQ Dev Biol. 2013 Aug 15;380(2):324-34. doi: 10.1016/j.ydbio.2013.05.022. Epub 2013 May 27.
The primary axis of cnidarians runs from the oral pole to the apical tuft and defines the major body axis of both the planula larva and adult polyp. In the anthozoan cnidarian Nematostella vectensis, the primary oral-aboral (O-Ab) axis first develops during the early embryonic stage. Here, we present evidence that pharmaceutical activators of canonical wnt signaling affect molecular patterning along the primary axis of Nematostella. Although not overtly morphologically complex, molecular investigations in Nematostella reveal that the O-Ab axis is demarcated by the expression of differentially localized signaling molecules and transcription factors that may serve roles in establishing distinct ectodermal domains. We have further characterized the larval epithelium by determining the position of a nested set of molecular boundaries, utilizing several newly characterized as well as previously reported epithelial markers along the primary axis. We have assayed shifts in their position in control embryos and in embryos treated with the pharmacological agents alsterpaullone and azakenpaullone, Gsk3β inhibitors that act as canonical wnt agonists, and the Wnt antagonist iCRT14, following gastrulation.
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CAS 676596-65-9 1-Azakenpaullone

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