WIKI4Inhibitor of Wnt/ß-Catenin signaling and tankyrase CAS# 838818-26-1 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 838818-26-1 | SDF | Download SDF |
| PubChem ID | 2984337 | Appearance | Powder |
| Formula | C29H23N5O3S | M.Wt | 521.59 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 6.8 mg/mL (13.04 mM; Need ultrasonic and warming) | ||
| Chemical Name | 2-[3-[[4-(4-methoxyphenyl)-5-pyridin-4-yl-1,2,4-triazol-3-yl]sulfanyl]propyl]benzo[de]isoquinoline-1,3-dione | ||
| SMILES | COC1=CC=C(C=C1)N2C(=NN=C2SCCCN3C(=O)C4=CC=CC5=C4C(=CC=C5)C3=O)C6=CC=NC=C6 | ||
| Standard InChIKey | RNUXIZKXJOGYQP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C29H23N5O3S/c1-37-22-11-9-21(10-12-22)34-26(20-13-15-30-16-14-20)31-32-29(34)38-18-4-17-33-27(35)23-7-2-5-19-6-3-8-24(25(19)23)28(33)36/h2-3,5-16H,4,17-18H2,1H3 | ||
| 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 | Inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM). Inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM); prevents the ubiquitination and degradation of axin. |
WIKI4 Dilution Calculator
WIKI4 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9172 mL | 9.5861 mL | 19.1721 mL | 38.3443 mL | 47.9304 mL |
| 5 mM | 0.3834 mL | 1.9172 mL | 3.8344 mL | 7.6689 mL | 9.5861 mL |
| 10 mM | 0.1917 mL | 0.9586 mL | 1.9172 mL | 3.8344 mL | 4.793 mL |
| 50 mM | 0.0383 mL | 0.1917 mL | 0.3834 mL | 0.7669 mL | 0.9586 mL |
| 100 mM | 0.0192 mL | 0.0959 mL | 0.1917 mL | 0.3834 mL | 0.4793 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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Inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM). Inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM); prevents the ubiquitination and degradation of axin.
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WIKI4, a novel inhibitor of tankyrase and Wnt/ss-catenin signaling.[Pubmed:23227175]
PLoS One. 2012;7(12):e50457.
The Wnt/ss-catenin signaling pathway controls important cellular events during development and often contributes to disease when dysregulated. Using high throughput screening we have identified a new small molecule inhibitor of Wnt/ss-catenin signaling, WIKI4. WIKI4 inhibits expression of ss-catenin target genes and cellular responses to Wnt/ss-catenin signaling in cancer cell lines as well as in human embryonic stem cells. Furthermore, we demonstrate that WIKI4 mediates its effects on Wnt/ss-catenin signaling by inhibiting the enzymatic activity of TNKS2, a regulator of AXIN ubiquitylation and degradation. While TNKS has previously been shown to be the target of small molecule inhibitors of Wnt/ss-catenin signaling, WIKI4 is structurally distinct from previously identified TNKS inhibitors.
Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4.[Pubmed:23762361]
PLoS One. 2013 Jun 6;8(6):e65404.
Recently a novel inhibitor of Wnt signaling was discovered. The compound, WIKI4, was found to act through tankyrase inhibition and regulate beta-catenin levels in many cancer cell lines and human embryonic stem cells. Here we confirm that WIKI4 is a high potency tankyrase inhibitor and that it selectively inhibits tankyrases over other ARTD enzymes tested. The binding mode of the compound to tankyrase 2 was determined by protein X-ray crystallography to 2.4 A resolution. The structure revealed a novel binding mode to the adenosine subsite of the donor NAD(+) binding groove of the catalytic domain. Our results form a structural basis for further development of potent and selective tankyrase inhibitors based on the WIKI4 scaffold.
