WIKI4 - CAS 838818-26-1
Catalog number: 838818-26-1
Category: Inhibitor
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Molecular Formula:
C29H23N5O3S
Molecular Weight:
521.595
COA:
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Targets:
Wnt
Description:
WIKI4 is a novel inhibitor of tankyrase and Wnt/ß-catenin signaling. 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. WIKI4 mediates its effects on Wnt/ß-catenin signaling by inhibiting the enzymatic activity of TNKS2, a regulator of AXIN ubiquitylation and degradation.
Purity:
0.98
Appearance:
white to off-white solid
Synonyms:
WIKI 4; WIKI-4
MSDS:
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InChIKey:
RNUXIZKXJOGYQP-UHFFFAOYSA-N
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
Canonical SMILES:
COC1=CC=C(C=C1)N2C(=NN=C2SCCCN3C(=O)C4=CC=CC5=C4C(=CC=C5)C3=O)C6=CC=NC=C6
1.Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4.
Haikarainen T1, Venkannagari H, Narwal M, Obaji E, Lee HW, Nkizinkiko Y, Lehtiö L. PLoS One. 2013 Jun 6;8(6):e65404. doi: 10.1371/journal.pone.0065404. Print 2013.
Recently a novel inhibitor of Wnt signaling was discovered. The compound, WIKI4, was found to act through tankyrase inhibition and regulate β-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 Å 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.
2.WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling.
James RG1, Davidson KC, Bosch KA, Biechele TL, Robin NC, Taylor RJ, Major MB, Camp ND, Fowler K, Martins TJ, Moon RT. PLoS One. 2012;7(12):e50457. doi: 10.1371/journal.pone.0050457. Epub 2012 Dec 5.
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.
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CAS 838818-26-1 WIKI4

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