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1-Azakenpaullone
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
1-Azakenpaullone图片
CAS NO:676596-65-9
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议

产品介绍
1-Azakenpaullon (1-Akp) 是一种高选择性和 ATP 竞争性的糖原合酶激酶 3 β (GSK-3β) 抑制剂，IC50 值为 18 nM。
Cas No.676596-65-9
别名1-氮杂坎帕罗酮,1-Akp
Canonical SMILESC1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br
分子式C15H10BrN3O
分子量328.16
溶解度≥ 15.05mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.