For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I010741 |
| CAS Number | 944328-88-5 |
| Synonyms | (2S)-2-[[2-(2,3-dihydro-1H-inden-5-yloxy)-9-[(4-phenylphenyl)methyl]purin-6-yl]amino]-3-phenylpropan-1-ol |
| Molecular Formula | C36H33N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C36H33N5O2/c42-23-31(20-25-8-3-1-4-9-25)38-34-33-35(40-36(39-34)43-32-19-18-28-12-7-13-30(28)21-32)41(24-37-33)22-26-14-16-29(17-15-26)27-10-5-2-6-11-27/h1-6,8-11,14-19,21,24,31,42H,7,12-13,20,22-23H2,(H,38,39,40)/t31-/m0/s1 |
| InChIKey | DOKZLKDGUQWMSX-HKBQPEDESA-N |
| SMILES | C1CC2=C(C1)C=C(C=C2)OC3=NC(=C4C(=N3)N(C=N4)CC5=CC=C(C=C5)C6=CC=CC=C6)NC(CC7=CC=CC=C7)CO |
| 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. |
