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1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death.