| Bioactivity | 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]. | ||||||||||||
| Target | EC50: 1.5 µM (ARFGAP1) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | QS11 | ||||||||||||
| CAS | 944328-88-5 | ||||||||||||
| Formula | C36H33N5O2 | ||||||||||||
| Molar Mass | 567.68 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |