Description
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.
Product information
CAS Number: 944328-88-5
Molecular Weight: 567.68
Formula: C36H33N5O2
Chemical Name: (2S)-2-{[9-({[1,1'-biphenyl]-4-yl}methyl)-2-(2,3-dihydro-1H-inden-5-yloxy)-9H-purin-6-yl]amino}-3-phenylpropan-1-ol
Smiles: OC[C@H](CC1C=CC=CC=1)NC1N=C(N=C2C=1N=CN2CC1C=CC(=CC=1)C1C=CC=CC=1)OC1C=C2CCCC2=CC=1
InChiKey: DOKZLKDGUQWMSX-HKBQPEDESA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 100 mg/mL (176.16 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
QS11 binds and inhibits the GTPase activating protein of ARFGAP1, suggesting that QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. 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. QS11 shows potent activity (EC50=0.5 μM) with little cytotoxicity toward HEK293 and human primary fibroblast cells. QS11 effectively reduces in vitro migration of metastatic human breast cancer cells.
Products are for research use only. Not for human use.
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