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QS11

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Chemical Structure| 944328-88-5 同义名 : QS11 free
CAS号 : 944328-88-5
货号 : A820510
分子式 : C36H33N5O2
纯度 : 99%+
分子量 : 567.679
MDL号 : MFCD18086864
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(184.96 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.81mL

1.76mL

0.88mL

17.62mL

3.52mL

1.76mL
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