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1-Azakenpaullone is a selective and cell-permeable inhibitor of glycogen synthase kinase-3β (GSK-3β) with IC50 value of 18nM [1, 2].

1-Azakenpaullone is a kenpaullone derivative with a modified heterocyclic basic structure. It shows potent inhibitory activity against GSK-3β over CDK1/cyclin B and CDK5/p25. The IC50 values for CDK1/cyclin B, CDK5/p25 and GSK-3β are 2μM, 4.2μM and 18nM, respectively. As an inhibitor of GSK-3β, 1-Azakenpaullone is developed as potential antidiabetic drug. 1-Azakenpaullone is found to protect rat insulinoma cell line INS-1E cells from glucolipotoxicity and stimulate cell proliferation. Besides that, 1-Azakenpaullone promotes the replication of beta cells in isolated rat islets at concentration of 1μM. In addition, 1-Azakenpaullone is reported to have effect in changing cardiac myocyte morphology. It increases cell area primarily through the elongation of the cells [1, 2 and 3].

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