QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC₅₀ of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells^[1].

EC50: 1.5 µM (ARFGAP1)^[1]

QS11 binds and inhibits the GTPase activating protein of ARFGAP1, suggesting that QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking^[1].
QS11 (2.5 μM) activates the Super(8X)TOPFlash reporter 200-fold in the presence of Wnt-3a conditioned medium, whereas Wnt-3a treatment alone increases reporter activity 40-fold^[2].
QS11 shows potent activity (EC₅₀=0.5 μM) with little cytotoxicity toward HEK293 and human primary fibroblast cells^[2].
QS11 effectively reduces in vitro migration of metastatic human breast cancer cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

567.68

C₃₆H₃₃N₅O₂

944328-88-5

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 100 mg/mL (176.16 mM)

* “≥” means soluble, but saturation unknown.

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Manish K. Singh, et al. Structure-activity Relationship Studies of QS11, a Small Molecule Wnt Synergistic Agonist. Bioorg Med Chem Lett. 2015 Nov 1; 25(21): 4838–4842.

  [2]. Zhang Q, et al. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7444-8.

ARF-GTP levels are measured by using the GGA binding assay. NIH 3T3 cells are treated with QS11 or QS11-NC at the indicated concentrations for 36 h. Cells are lysed in ARF assay lysis buffer [50 mM Tris·HCl (pH 7.5), 100 mM NaCl, 2 mM MgCl₂, 0.1% SDS, 0.5% sodium deoxycholate, 1% Triton X-100, 10% glycerol, and protease inhibitors]. GTP-bound ARF is assayed by its binding to a GST fusion protein, which contains the VHS domain to the GAT region of an ARF effector GGA3^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Manish K. Singh, et al. Structure-activity Relationship Studies of QS11, a Small Molecule Wnt Synergistic Agonist. Bioorg Med Chem Lett. 2015 Nov 1; 25(21): 4838–4842.

  [2]. Zhang Q, et al. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7444-8.