WIKI4

Inhibitor of Wnt/ß-Catenin signaling and tankyrase CAS# 838818-26-1

WIKI4

2D Structure

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3D structure

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WIKI4

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Chemical Properties of WIKI4

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.
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.
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.

Biological Activity of WIKI4

DescriptionInhibitor 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

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WIKI4 Molarity Calculator

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Preparing Stock Solutions of WIKI4

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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Background on WIKI4

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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References on WIKI4

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.

Description

WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.

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