EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72392_C
激活素/BMP/TGF-β通路抑制剂；抑制ALK5
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总览
RepSox 是一种可穿透细胞的 TGF-β 1 型受体 (TGFβRI) ALK5 选择性抑制剂（ALK5 自身磷酸化、TGF-β 细胞实验和 HepG2 细胞中 ALK5 结合的 IC₅₀ 分别为 4 nM、18 nM 和 23 nM（Gellibert et al.）)。该抑制剂对 9 种相关激酶（包括 p38 MAPK 和 GSK3）表现出较弱的活性（IC₅₀ > 16 μM）（Gellibert et al.）。本品以分子的盐酸盐形式供应。
重编程
·增强用OCT4、KLF4和c-MYC转导的小鼠胚胎成纤维细胞（mef）的重编程 (Ichida et al.; Subramanyam et al.)
·结合CHIR99021、丙戊酸、Forskolin、SP600125、Gö6983和Y-27632，将成纤维细胞直接谱系重编程为成熟神经元（Hu et al.）。
分化
·单独使用或与福斯克林、地塞米松和烟酰胺联合使用，诱导人胰腺祖细胞分化为产生胰岛素的细胞（Kunisada et al.; Rezania et al.)。
细胞类型
神经元，成骨细胞，胰腺细胞，多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化，重编程
研究领域
上皮细胞研究，干细胞生物学
CAS 编号
2319939-07-4
化学式
C₁₇H₁₃N₅ · HCl
纯度
≥98%
通路
Activin/Nodal/TGFβ
靶点
ALK5
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。
应用领域
本产品专为以下研究领域设计，适用于工作流程中的高亮阶段。探索这些工作流程，了解更多我们为各研究领域提供的其他配套产品。
相关材料与文献
技术资料 (3)
文献 (6)
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Journal of medicinal chemistry 2004 AUG
Abstract
Optimization of the screening hit 1 led to the identification of novel 1,5-naphthyridine aminothiazole and pyrazole derivatives,which are potent and selective inhibitors of the transforming growth factor-beta type I receptor,ALK5. Compounds 15 and 19,which inhibited ALK5 autophosphorylation with IC50 = 6 and 4 nM,respectively,showed potent activities in both binding and cellular assays and exhibited selectivity over p38 mitogen-activated protein kinase. The X-ray crystal structure of 19 in complex with human ALK5 is described,confirming the binding mode proposed from docking studies.
A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog.
Cell stem cell 2009 NOV
Abstract
The combined activity of three transcription factors can reprogram adult cells into induced pluripotent stem cells (iPSCs). However,the transgenic methods used for delivering reprogramming factors have raised concerns regarding the future utility of the resulting stem cells. These uncertainties could be overcome if each transgenic factor were replaced with a small molecule that either directly activated its expression from the somatic genome or in some way compensated for its activity. To this end,we have used high-content chemical screening to identify small molecules that can replace Sox2 in reprogramming. We show that one of these molecules functions in reprogramming by inhibiting Tgf-beta signaling in a stable and trapped intermediate cell type that forms during the process. We find that this inhibition promotes the completion of reprogramming through induction of the transcription factor Nanog.
Production of functional glucagon-secreting α-cells from human embryonic stem cells.
Diabetes 2011 JAN
Abstract
OBJECTIVE: Differentiation of human embryonic stem (hES) cells to fully developed cell types holds great therapeutic promise. Despite significant progress,the conversion of hES cells to stable,fully differentiated endocrine cells that exhibit physiologically regulated hormone secretion has not yet been achieved. Here we describe an efficient differentiation protocol for the in vitro conversion of hES cells to functional glucagon-producing α- cells. RESEARCH DESIGN AND METHODS: Using a combination of small molecule screening and empirical testing,we developed a six-stage differentiation protocol for creating functional α-cells. An extensive in vitro and in vivo characterization of the differentiated cells was performed. RESULTS: A high rate of synaptophysin expression (textgreater75%) and robust expression of glucagon and the α-cell transcription factor ARX was achieved. After a transient polyhormonal state in which cells coexpress glucagon and insulin,maturation in vitro or in vivo resulted in depletion of insulin and other β-cell markers with concomitant enrichment of α-cell markers. After transplantation,these cells secreted fully processed,biologically active glucagon in response to physiologic stimuli including prolonged fasting and amino acid challenge. Moreover,glucagon release from transplanted cells was sufficient to reduce demand for pancreatic glucagon,resulting in a significant decrease in pancreatic α-cell mass. CONCLUSIONS: These results indicate that fully differentiated pancreatic endocrine cells can be created via stepwise differentiation of hES cells. These cells may serve as a useful screening tool for the identification of compounds that modulate glucagon secretion as well as those that promote the transdifferentiation of α-cells to β-cells.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 2319939-07-4 |
| Chemical Formula | C₁₇H₁₃N₅ · HCl |
| 纯度 | ≥ 98% |
| Target | ALK5 |
| Pathway | Activin/Nodal/TGFβ |
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