EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73172_C
Hedgehog通路激活剂；激活Smoothened (SMO)蛋白
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总览
GSA 10是Smoothened （SMO）的激动剂，SMO是一种细胞表面受体和hedgehog信号通路的介导因子。它是一种喹啉甲酰胺衍生物，其结合位点不同于cyclopamine。在基于碱性磷酸酶的小鼠间质细胞系（C3H10T1/2）分化试验中，GSA10在EC₅₀为1.2 μM时具有活性（Gorojankina等人）。
分化
·促进多能间充质祖细胞向成骨细胞的分化（Gorojankina等人）。
别名
Not applicable
细胞类型
间充质干/祖细胞，成骨细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
应用
分化
研究领域
干细胞生物学
CAS 编号
300833-95-8
化学式
C₂₆H₃₀N₂O₅
分子量
450.5 克/摩尔
纯度
≥ 95 %
通路
Hedgehog
靶点
SMO
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 (1)
Discovery, molecular and pharmacological characterization of GSA-10, a novel small-molecule positive modulator of Smoothened. Molecular pharmacology 2013
Abstract
Activation of the Smoothened (Smo) receptor mediates Hedgehog (Hh) signaling. Hh inhibitors are in clinical trials for cancer, and small-molecule Smo agonists may have therapeutic interests in regenerative medicine. Here, we have generated and validated a pharmacophoric model for Smo agonists and used this model for the virtual screening of a library of commercially available compounds. Among the 20 top-scoring ligands, we have identified and characterized a novel quinolinecarboxamide derivative, propyl 4-(1-hexyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamido) benzoate, (GSA-10), as a Smo agonist. GSA-10 fits to the agonist pharmacophoric model with two hydrogen bond acceptor groups and four hydrophobic regions. Using pharmacological, biochemical, and molecular approaches, we provide compelling evidence that GSA-10 acts at Smo to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts. However, this molecule does not display the hallmarks of reference Smo agonists. Remarkably, GSA-10 does not recognize the classic bodipy-cyclopamine binding site. Its effect on cell differentiation is inhibited by Smo antagonists, such as MRT-83, SANT-1, LDE225, and M25 in the nanomolar range, by GDC-0449 in the micromolar range, but not by cyclopamine and CUR61414. Thus, GSA-10 allows the pharmacological characterization of a novel Smo active site, which is notably not targeted to the primary cilium and strongly potentiated by forskolin and cholera toxin. GSA-10 belongs to a new class of Smo agonists and will be helpful for dissecting Hh mechanism of action, with important implications in physiology and in therapy.
更多信息
| Molecular Weight | 450.5 g/mol |
|---|---|
| 种属 | Human, Mouse, Non-Human Primate, Other, Rat |
| Alternative Names | Not applicable |
| Cas Number | 300833-95-8 |
| Chemical Formula | C₂₆H₃₀N₂O₅ |
| 纯度 | ≥ 95% |
| Target | SMO |
| Pathway | Hedgehog |
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