EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73322_C
WNT通路激活剂；GSK3抑制
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总览
BIO-Acetoxime是GSK3抑制剂BIO（产品号 #72032）的类似物。它强效抑制GSK3α和GSK3β（IC₅₀=10 nM），对细胞周期依赖性蛋白激酶Cdk5/p25、Cdk2/A和Cdk1/B（IC₅₀分别为2.4、4.3和63 μM）的抑制作用较弱（Meijer等；Polychronopoulos等）。通过抑制GSK3β，BIO-Acetoxime可阻断β-catenin的磷酸化和降解，从而激活WNT通路调控基因的转录（Meijer等）。
免疫学
·抑制CD8+效应T细胞分化（Zhou等）。
·抑制病毒基因表达并保护口腔上皮细胞免受单纯疱疹病毒1型感染（Hsu和Hung）。
细胞类型
T 细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
研究领域
免疫
CAS 编号
740841-15-0
化学式
C₁₈H₁₂BrN₃O₃
纯度
≥ 95 %
通路
WNT
靶点
GSK3
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
技术资料 (1)
文献 (4)
Antiherpetic potential of 6-bromoindirubin-3'-acetoxime (BIO-acetoxime) in human oral epithelial cells. Archives of virology 2013 JUN
Abstract
Glycogen synthase kinase 3 (GSK-3) functions in the regulation of glycogen metabolism, in the cell cycle, and in immune responses and is targeted by some viruses to favor the viral life cycle. Inhibition of GSK-3 by 6-bromoindirubin-3'-acetoxime (BIO-acetoxime), a synthetic derivative of a compound from the Mediterranean mollusk Hexaplex trunculus, protects cells from varicella infection. In this study, we examined the effects of BIO-acetoxime against herpes simplex virus-1 (HSV-1) infection in human oral epithelial cells, which represent a natural target cell type. The results revealed that BIO-acetoxime relieves HSV-1-induced cytopathic effects and apoptosis. We also found that BIO-acetoxime reduced viral yields and the expression of different classes of viral proteins. Furthermore, addition of BIO-acetoxime before, simultaneously with or after HSV-1 infection significantly reduced viral yields. Collectively, BIO-acetoxime may suppress viral gene expression and protect oral epithelial cells from HSV-1 infection. These results suggest the possible involvement of GSK-3 in HSV-1 infection.
Differentiation and persistence of memory CD8(+) T cells depend on T cell factor 1. Immunity 2010 AUG
Abstract
T cell factor 1 (TCF-1) is a transcription factor known to act downstream of the canonical Wnt pathway and is essential for normal T cell development. However, its physiological roles in mature CD8(+) T cell responses are unknown. Here we showed that TCF-1 deficiency limited proliferation of CD8(+) effector T cells and impaired their differentiation toward a central memory phenotype. Moreover, TCF-1-deficient memory CD8(+) T cells were progressively lost over time, exhibiting reduced expression of the antiapoptotic molecule Bcl-2 and interleukin-2 receptor beta chain and diminished IL-15-driven proliferation. TCF-1 was directly associated with the Eomes allele and the Wnt-TCF-1 pathway was necessary and sufficient for optimal Eomes expression in naive and memory CD8(+) T cells. Importantly, forced expression of Eomes partly protected TCF-1-deficient memory CD8(+) T cells from time-dependent attrition. Our studies thus identify TCF-1 as a critical player in a transcriptional program that regulates memory CD8 differentiation and longevity.
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. Journal of medicinal chemistry 2004 FEB
Abstract
Pharmacological inhibitors of glycogen synthase kinase-3 (GSK-3) and cyclin-dependent kinases have a promising potential for applications against several neurodegenerative diseases such as Alzheimer's disease. Indirubins, a family of bis-indoles isolated from various natural sources, are potent inhibitors of several kinases, including GSK-3. Using the cocrystal structures of various indirubins with GSK-3beta, CDK2 and CDK5/p25, we have modeled the binding of indirubins within the ATP-binding pocket of these kinases. This modeling approach provided some insight into the molecular basis of indirubins' action and selectivity and allowed us to forecast some improvements of this family of bis-indoles as kinase inhibitors. Predicted molecules, including 6-substituted and 5,6-disubstituted indirubins, were synthesized and evaluated as CDK and GSK-3 inhibitors. Control, kinase-inactive indirubins were obtained by introduction of a methyl substitution on N1.
更多信息
| 种属 | Human, Mouse, Non-Human Primate, Other, Rat |
|---|---|
| Cas Number | 740841-15-0 |
| Chemical Formula | C₁₈H₁₂BrN₃O₃ |
| 纯度 | ≥ 95% |
| Target | GSK3 |
| Pathway | WNT |
