产品号 #72392_C
激活素/BMP/TGF-β通路抑制剂；抑制ALK5
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，其它细胞系，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
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
Applications
This product is designed for use in the following research area(s) as part of the highlighted workflow stage(s). Explore these workflows to learn more about the other products we offer to support each research area.
Resources and Publications
Educational Materials (3)
Publications (6)
Direct Conversion of Normal and Alzheimer's Disease Human Fibroblasts into Neuronal Cells by Small Molecules. Cell stem cell 2015 AUG
Abstract
Neuronal conversion from human fibroblasts can be induced by lineage-specific transcription factors; however, the introduction of ectopic genes limits the therapeutic applications of such induced neurons (iNs). Here, we report that human fibroblasts can be directly converted into neuronal cells by a chemical cocktail of seven small molecules, bypassing a neural progenitor stage. These human chemical-induced neuronal cells (hciNs) resembled hiPSC-derived neurons and human iNs (hiNs) with respect to morphology, gene expression profiles, and electrophysiological properties. This approach was further applied to generate hciNs from familial Alzheimer's disease patients. Taken together, our transgene-free and chemical-only approach for direct reprogramming of human fibroblasts into neurons provides an alternative strategy for modeling neurological diseases and for regenerative medicine.
Small molecules induce efficient differentiation into insulin-producing cells from human induced pluripotent stem cells. Stem cell research 2012 MAR
Abstract
Human induced pluripotent stem (hiPS) cells have potential uses for drug discovery and cell therapy, including generation of pancreatic β-cells for diabetes research and treatment. In this study, we developed a simple protocol for generating insulin-producing cells from hiPS cells. Treatment with activin A and a GSK3β inhibitor enhanced efficient endodermal differentiation, and then combined treatment with retinoic acid, a bone morphogenic protein inhibitor, and a transforming growth factor-β (TGF-β) inhibitor induced efficient differentiation of pancreatic progenitor cells from definitive endoderm. Expression of the pancreatic progenitor markers PDX1 and NGN3 was significantly increased at this step and most cells were positive for anti-PDX1 antibody. Moreover, several compounds, including forskolin, dexamethasone, and a TGF-β inhibitor, were found to induce the differentiation of insulin-producing cells from pancreatic progenitor cells. By combined treatment with these compounds, more than 10% of the cells became insulin positive. The differentiated cells secreted human c-peptide in response to various insulin secretagogues. In addition, all five hiPS cell lines that we examined showed efficient differentiation into insulin-producing cells with this protocol.
Multiple targets of miR-302 and miR-372 promote reprogramming of human fibroblasts to induced pluripotent stem cells. Nature biotechnology 2011 MAY
Abstract
The embryonic stem cell-specific cell cycle-regulating (ESCC) family of microRNAs (miRNAs) enhances reprogramming of mouse embryonic fibroblasts to induced pluripotent stem cells. Here we show that the human ESCC miRNA orthologs hsa-miR-302b and hsa-miR-372 promote human somatic cell reprogramming. Furthermore, these miRNAs repress multiple target genes, with downregulation of individual targets only partially recapitulating the total miRNA effects. These targets regulate various cellular processes, including cell cycle, epithelial-mesenchymal transition (EMT), epigenetic regulation and vesicular transport. ESCC miRNAs have a known role in regulating the unique embryonic stem cell cycle. We show that they also increase the kinetics of mesenchymal-epithelial transition during reprogramming and block TGFβ-induced EMT of human epithelial cells. These results demonstrate that the ESCC miRNAs promote dedifferentiation by acting on multiple downstream pathways. We propose that individual miRNAs generally act through numerous pathways that synergize to regulate and enforce cell fate decisions.
更多信息
| Species | Human, Mouse, Non-Human Primate, Other, Rat |
|---|---|
| Cas Number | 2319939-07-4 |
| Chemical Formula | C₁₇H₁₃N₅ · HCl |
| Purity | ≥ 98% |
| Target | ALK5 |
| Pathway | Activin/Nodal/TGFβ |
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