1-Azakenpaullone
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52972ES05
2 mg
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¥ 1795.00
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52972ES08
5 mg
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¥ 2875.00
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52972ES10
10 mg
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¥ 4595.00
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1-Azakenpaullone是高效的、细胞渗透性和ATP竞争性的糖原合酶激酶-3β (GSK-3β)抑制剂(IC50值为18 nM),并且对GSK-3β的抑制效果是CDK1和 CDK5的100倍以上。同时,1-Azakenpaullone可应用于抗糖尿病药物的开发 

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参考文献

[1]. Shin S, et al. Glycogen synthase kinase-3β positively regulates protein synthesis and cell proliferation through the regulation of translation initiation factor 4E-binding protein 1. Oncogene. 2014 Mar 27;33(13):1690-9.

[2]. Lee HW, et al. High-content screening assay-based discovery of paullones as novel podocyte-protective agents. Am J Physiol Renal Physiol. 2018 Feb 1;314(2): F280-F292.

[3] Liu H, 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.

[4] Duffy DJ, et al. GSK3 inhibitors regulate MYCN mRNA levels and reduce neuroblastoma cell viability through multiple mechanisms, including p53 and Wnt signaling. Mol Cancer Ther. 2014 Feb;13(2):454-67.

[5] Kunick C, 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.

 

存储条件

冰袋运输。粉末直接保存于-20℃,有效期2年。建议分装后-20℃避光保存,避免反复冻融。

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