QS 11Wnt synergistic agonist CAS# 944328-88-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 944328-88-5 | SDF | Download SDF |
| PubChem ID | 42623900 | Appearance | Powder |
| Formula | C36H33N5O2 | M.Wt | 567.68 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol | ||
| Chemical Name | (2S)-2-[[2-(2,3-dihydro-1H-inden-5-yloxy)-9-[(4-phenylphenyl)methyl]purin-6-yl]amino]-3-phenylpropan-1-ol | ||
| SMILES | C1CC2=C(C1)C=C(C=C2)OC3=NC4=C(C(=N3)NC(CC5=CC=CC=C5)CO)N=CN4CC6=CC=C(C=C6)C7=CC=CC=C7 | ||
| Standard InChIKey | DOKZLKDGUQWMSX-HKBQPEDESA-N | ||
| Standard 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. Modulates ARF-GTP levels and synergizes with the Wnt/β-catenin signaling pathway to upregulate β-catenin nuclear translocation. Also reduces in vitro migration of metastatic human breast cancer cells. |
QS 11 Dilution Calculator
QS 11 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.7616 mL | 8.8078 mL | 17.6156 mL | 35.2311 mL | 44.0389 mL |
| 5 mM | 0.3523 mL | 1.7616 mL | 3.5231 mL | 7.0462 mL | 8.8078 mL |
| 10 mM | 0.1762 mL | 0.8808 mL | 1.7616 mL | 3.5231 mL | 4.4039 mL |
| 50 mM | 0.0352 mL | 0.1762 mL | 0.3523 mL | 0.7046 mL | 0.8808 mL |
| 100 mM | 0.0176 mL | 0.0881 mL | 0.1762 mL | 0.3523 mL | 0.4404 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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EC50: 1.5 μM for ARFGAP1 enzymatic assay [1] and 0.5 μM for Wnt synergist [2]
Purine derivative QS11 is a Wnt synergistic agonist by inhibiting the GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1). ARFGAP1 promotes hydrolysis of ARF1-bound GTP and is required in membrane trafficking and /or vesicle transport.
In vitro: QS11 showed potent Wnt Synergist activity with little cytotoxicity in HEK293 cells (EC50 = 0.5 μM) and human primary fibroblast cells (EC50 ≥ 10 μM). QS11 at 2.5 μM activated the Super(8X)TOPFlash reporter ~200-fold in the presence of Wnt-3a conditioned medium. Synergistic effect was also observed when QS11 was combined with recombinant Wnt-3a protein (10–200 ng/ml) [2].
In vivo: In Wnt signaling test model, embryos were injected with QS11, XWnt-8 RNA or a combination of QS11and XWnt-8 RNA. Compared with QS11 alone and XWnt-8 RNA alone, injection of a combination of XWnt-8 RNA and QS11 induced significantly more full (20.9%) and partial (30.2%) double axis formation [2]..
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Singh MK1, Gao H1, Sun W1, Song Z1, Schmalzigaug R2, Premont RT2, Zhang Q3. Structure-activity relationship studies of QS11, a small molecule Wnt synergistic agonist. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4838-42.
[2] Zhang Q1, Major MB, Takanashi S, Camp ND, Nishiya N, Peters EC, Ginsberg MH, Jian X, Randazzo PA, Schultz PG, Moon RT, Ding S. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7444-8. Epub 2007 Apr 25.
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The effect of special training for quinacrine sterilization (QS) in Faisalabad, Pakistan: a report on an 1833-women subset of 11,000 cases.[Pubmed:14763188]
Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S67-71.
OBJECTIVE: To determine the impact of retrained clinicians on the efficacy of transcervical quinacrine sterilization. METHOD: Retraining of clinicians in the accepted insertion technique was conducted in 1996. From 1 January 1997 through 2001, they performed 1089 quinacrine sterilizations in 11 MCH clinics of the Mother & Child Welfare Association at Faisalabad, Pakistan. Of these, 885 women had a recorded follow-up visit (81.4%) by 31 December 2001. RESULT: Reported pregnancy failures declined after retraining from 5.4% (SE 2.3) for one year of use to 1.1% (SE 0.4) for 5 years of use. The rates at 4 years of use showed the expected increase in failures for women 30 years old or younger of 1.5% (SE 0.7) compared to 0.9% (SE 0.4) for those over 30; a lower rate of 0.8% (SE 0.4) for breastfeeding subjects and 2.2% (SE 1.1) for mothers not breastfeeding; but rates were similar for uterine length and post insertion traumatic bleeding. CONCLUSION: Quinacrine sterilization appears safe with acceptable efficacy.
A chemical approach to stem cell biology.[Pubmed:17493865]
Curr Opin Chem Biol. 2007 Jun;11(3):252-8.
Small molecule libraries have been used successfully to probe several biological systems. Recent work has translated these successes across to the field of stem cell biology. Stem cells hold promise for both modeling of early development as well as having therapeutic potential. Enhanced understanding of the molecular mechanisms that control stem cell fates as well as an improved ability to manipulate cell populations are required. Known mechanistic chemical compounds have been used with stem cells to accomplish these two goals. More recently, through the utilization of high fitness libraries in phenotype-based screens, several small molecules that control self-renewal and differentiation in stem cells have been identified. These small molecules provide useful chemical tools for both basic research and practical applications.
Small-molecule synergist of the Wnt/beta-catenin signaling pathway.[Pubmed:17460038]
Proc Natl Acad Sci U S A. 2007 May 1;104(18):7444-8.
The Wnt/beta-catenin signaling pathway regulates cell fate and behavior during embryogenesis, adult tissue homeostasis, and regeneration. When inappropriately activated, the pathway has been linked to colorectal cancer and melanoma, and when attenuated it may contribute to Alzheimer's disease and osteoporosis. Small molecules that modulate Wnt signaling will likely provide new insights into the regulation of this key developmental pathway and ultimately provide pharmacological agents to control Wnt signaling in vivo. To this end, we screened a library of 100,000 small molecules for activity in a cell-based assay of Wnt/beta-catenin signaling and discovered a purine derivative, QS11, that synergizes with Wnt-3a ligand in the activation of Wnt/beta-catenin signal transduction. Through affinity chromatography and subsequent functional assays, we showed that QS11 binds and inhibits the GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1), suggesting that QS11 modulates Wnt/beta-catenin signaling through an effect on protein trafficking. Consistent with its function as an ARFGAP inhibitor, QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
