1-Azakenpaullone
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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
