1-Azakenpaullone

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Chemical Structure| 676596-65-9 同义名 : 1-Akp
CAS号 : 676596-65-9
货号 : A192559
分子式 : C15H10BrN3O
纯度 : 99%+
分子量 : 328.16
MDL号 : MFCD09037522
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • GSK-3β

    GSK-3β, IC50:18 nM

  • GSK-3β

    GSK-3β, IC50:18 nM
描述 Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase involved in cell differentiation, cellular growth and proliferation, apoptosis, and inflammation. There are two isoforms of GSK-3, GSK-3α and GSK-3β. 1-Azakenpaullone is a potent inhibitor of GSK-3β with an IC50 value of 18 nM. In contrast, the IC50 values of 1-Azakenpaullone against CDK1/cycline B and CDK5/p25 were 2.0 and 4.2 μM, respectively[3]. 1-Azakenpaullone at the concentrations of 5, 10, and 15 μM significantly promoted DNA synthesis in human pancreatic islets above the levels at 8 mM glucose. Exposure of human pancreatic islets to 8 mM glucose and 15 μM 1-Azakenpaullone significantly reduced cells in G0/G1 phase and increased cells in S phase. Combined treatment of human islets with 8 mM glucose and 5 μM 1-Azakenpaullone significantly increased Ki-67+/insulin+ cells as compared with basal glucose[4]. After 2-week administration of 1-Azakenpaullone, a significant reduction in the levels of phosphorylated Akt GSK-3β, and cyclin D1 was observed in the islets of c-KitW/+ mice when compared to c-Kit+/+ mice[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.30mL

15.24mL

3.05mL

1.52mL

30.47mL

6.09mL

3.05mL
参考文献

[1]Liu H, Remedi MS, et al. Glycogen synthase kinase-3 and mammalian target of rapamycin pathways contribute to DNA synthesis, cell cycle progression, and proliferation in human islets. Diabetes. 2009 Mar;58(3):663-72.

[2]Kunick C, Lauenroth K, et al. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.

[3]Kunick C, Lauenroth K, Leost M, Meijer L, Lemcke T. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6. doi: 10.1016/j.bmcl.2003.10.062. PMID: 14698171.

[4]Liu H, Remedi MS, Pappan KL, Kwon G, Rohatgi N, Marshall CA, McDaniel ML. Glycogen synthase kinase-3 and mammalian target of rapamycin pathways contribute to DNA synthesis, cell cycle progression, and proliferation in human islets. Diabetes. 2009 Mar;58(3):663-72. doi: 10.2337/db07-1208. Epub 2008 Dec 10. PMID: 19073772; PMCID: PMC2646065.

[5]Feng ZC, Donnelly L, Li J, Krishnamurthy M, Riopel M, Wang R. Inhibition of Gsk3β activity improves β-cell function in c-KitWv/+ male mice. Lab Invest. 2012 Apr;92(4):543-55. doi: 10.1038/labinvest.2011.200. Epub 2012 Jan 16. PMID: 22249311; PMCID: PMC3940483.