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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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 944328-88-5 |
分子式 | C36H33N5O2 |
分子量 | 567.679 |
别名 | QS11 free |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
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 |