|(S)-2-((9-([1,1'-联苯] -4-基甲基)-2-((2,3-二氢-1H-茚-5-基)氧基] -9H-嘌呤- 6-基)氨基)-3-苯基丙-1-醇|CsnPharm

CAS No.: 944328-88-5

QS11 Catalog No. CSN23762

Synonyms: Wnt Pathway Activator II

QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor that increases activity of ARFs in NIH3T3 cells at concentration of 1 μM, it also modulates Wnt/β-catenin signaling.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Both the Wnt/β-catenin signaling pathway and small GTPases of the ADP-ribosylation factors (ARF) family play important roles in regulating cell development, homeostasis and fate. QS11 is a small molecule Wnt synergist that binds to ARF GTPase-activating protein 1 (ARFGAP1) with an EC₅₀ value of 1.5 µM. In the ARFGAP1 enzymatic assay, QS11 at 10 and 20 µM inhibited the enzymatic activity by 67% and 90%, respectively^[1]. QS11 showed potent activity (EC₅₀ = 0.5 µM) with little cytotoxicity toward HEK293 and human primary fibroblast cells. QS11 (2.5 µM) activated the Super(8X) TOPFlash reporter 200-fold in the presence of Wnt-3a CM (conditioned medium). This synergistic effect was also observed when QS11 was combined with recombinant Wnt-3a protein (10 - 200 ng/mL). When tested in a transwell cell migration assay, QS11 inhibited the migration of MDA-MB-231 cells in a dose-dependent manner, with 80% of the migration inhibited at a concentration of 2.5 µM, compared with the DMSO control. In vivo, injection of a combination of XWnt-8 RNA and QS11 induced significantly more full (20.9%) and partial (30.2%) double axis formation further supporting the notion that QS11 acts as a synergistic Wnt agonist^[2].
参考文献

[1] Singh MK, Gao H, Sun W, et al. Structure-activity relationship studies of QS11, a small molecule Wnt synergistic agonist. Bioorg Med Chem Lett. 2015;25(21):4838-4842
[2] Zhang Q, Major MB, Takanashi S, et al. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A. 2007;104(18):7444-7448

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7616 mL
- 8.8078 mL
- 17.6156 mL
- 5 mM
- 0.3523 mL
- 1.7616 mL
- 3.5231 mL
- 10 mM
- 0.1762 mL
- 0.8808 mL
- 1.7616 mL

技术信息

CAS号

944328-88-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C36H33N5O2

运输

蓝冰

分子量

567.68

别名

Wnt Pathway Activator II

溶解度

DMSO	100.0 mg/mL (176.2 mM)
Water	Insoluble

动物实验配方

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QS11 Catalog No. CSN23762

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