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1-Azakenpaullone Sale

(Synonyms: 1-氮杂坎帕罗酮,1-Akp) 目录号 : GC13907

A potent inhibitor of GSK3β

1-Azakenpaullone Chemical Structure

Cas No.:676596-65-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,953.00
现货
2mg
¥1,080.00
现货
5mg
¥2,160.00
现货
10mg
¥3,600.00
现货

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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 676596-65-9 SDF
别名 1-氮杂坎帕罗酮,1-Akp
Canonical SMILES C1C2=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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.0473 mL 15.2365 mL 30.4729 mL
5 mM 0.6095 mL 3.0473 mL 6.0946 mL
10 mM 0.3047 mL 1.5236 mL 3.0473 mL
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