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GSA 10

Hedgehog通路激活剂;激活Smoothened (SMO)蛋白

产品号 #(选择产品)

产品号 #73172_C

Hedgehog通路激活剂;激活Smoothened (SMO)蛋白

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。

Document Type
Product Name
Catalog #
Lot #
Language
Product Name
GSA 10
Catalog #
73174
Lot #
All
Language
English
Document Type
Safety Data Sheet
Product Name
GSA 10
Catalog #
73174
Lot #
All
Language
English

应用领域

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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. Gorojankina T et al. 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

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
质量保证:

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