1-Azakenpaullone
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
1-Azakenpaullone是选择性和细胞渗透性糖原合酶激酶-3β (GSK-3β)抑制剂,IC50值为18 nM [1, 2].
1-Azakenpaullone是kenpaullone 的衍生物,具有一个修饰过的杂环基结构.其对GSK-3β的抑制活性高于CDK1/cyclin B和 CDK5/p25.对CDK1/cyclin B\CDK5/p25和GSK-3β的IC50值分别为2 μM\4.2 μM和18 nM.作为GSK-3β的抑制剂,1-Azakenpaullone已开发作为高效的抗糖尿病药物.1-Azakenpaullone能保护大鼠胰岛瘤细胞系INS-1E细胞抵抗糖脂毒性,并刺激细胞增殖.此外,1 μM 1-Azakenpaullone能促进分离的大鼠胰岛中β细胞增殖.1-Azakenpaullone能改变心肌细胞形态.1-Azakenpaullone主要通过延伸细胞以增加细胞面积[1, 2, 3].
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 328.16 |
Cas No. | 676596-65-9 |
Formula | C15H10BrN3O |
Solubility | insoluble in H2O; insoluble in EtOH; ≥15.05 mg/mL in DMSO |
SDF | Download SDF |
Canonical SMILES | C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | 1-Azakenpaullone是高效选择性GSK-3β抑制剂,IC50值为18 nM. | |||||
靶点 | GSK-3β | |||||
IC50 | 18 nM |
化学结构
![1-Azakenpaullone](http://www.apexbt.com//media/diy/images/struct/B3690.png)