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  • 1-Azakenpaullone
1-Azakenpaullone的可视化放大

1-Azakenpaullone

A potent inhibitor of GSK3β

原价
¥1300-4312
价格
1040-3450
1-Azakenpaullone的二维码

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  • 货号: ajci12056
  • CAS: 676596-65-9
  • 别名: 1-氮杂坎帕罗酮,1-Akp
  • 分子式: C15H10BrN3O
  • 分子量: 328.16
  • 纯度: >98%
  • 溶解度: ≥ 15.05mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

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].

参考文献:
[1] Kunick C, Lauenroth K, Leost M, et al. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β. Bioorganic & medicinal chemistry letters, 2004, 14(2): 413-416.
[2] Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.
[3] Markou T, Cullingford T E, Giraldo A, et al. Glycogen synthase kinases 3α and 3β in cardiac myocytes: regulation and consequences of their inhibition. Cellular signalling, 2008, 20(1): 206-218.

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