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1-Azakenpaullone

1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂，其 IC50=18 nM。

CAS号

676596-65-9

分子式

C15H10BrN3O

主要靶点

GSK-3

仅限科研使用

Cat No : CM14299

Print datasheet

Synonyms

azakenpaullone|1-氮杂坎帕罗酮

验证数据展示

  • CAS No.: 676596-65-9

    1-Azakenpaullone
    CAS#: 676596-65-9

产品信息

1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.

CAS号 676596-65-9
分子式 C15H10BrN3O
主要靶点 GSK-3
主要通路 PI3K/Akt/mTOR信号通路|干细胞
分子量 328.16
纯度 99.60%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 azakenpaullone|1-氮杂坎帕罗酮

靶点活性

GSK-3β:18 nM

体内活性

Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the ketamine-induced locomotor hyperactivity, disruption of PPI and cognitive de?cits, and improves the ketamine-induced motor incoordination in rotarod test. [5]

体外活性

1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. [1] In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. [2] 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death. [3][4]

溶解度

H2O:<1 mg/mL,DMSO:61 mg/mL (185.9 mM),Ethanol:<1 mg/mL

细胞实验

Cell replication is determined by BrdUrd incorporation after treatment with 1-Azakenpaullone for 24 h. The relative cell number is determined after treatment with 1-Azakenpaullone for 4 days using the CyQuant cell proliferation assay. Results are presented as fold change relative to control. (Only for Reference)

参考文献

1.Kunick C, et al. Bioorg Med Chem Lett. 2004, 14(2), 413-416.
2.Liu H, et al. Diabetes. 2009, 58(3), 663-672.
3.Stukenbrock H, et al. J Med Chem. 2008, 51(7), 2196-2207.
4.Mussmann R, et al. J Biol Chem. 2007, 282(16), 12030-12037.
5.Chan MH, et al. Schizophr Res. 2012, 136(1-3), 96-103.

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