XAV 939 - CAS 284028-89-3
Catalog number: B0084-212112
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C14H11F3N2OS
Molecular Weight:
312.31
COA:
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Targets:
Wnt | β-catenin | Tankyrase-1
Description:
XAV 939 is a tankyrase (TNKS) inhibitor with IC50 values of 11 nM and 4 nM for tankyrase 1 and 2 respectively. XAV 939 antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. It also suppresses proliferation of the μ-catenin-dependent colon carcinoma cell line DLD-1.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-212112 50 mg $168 In stock
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Appearance:
White to Pale Yellow Solid
Synonyms:
XAV939; XAV 939; XAV-939. 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
MSDS:
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Melting Point:
>230°C (dec.)
InChIKey:
KLGQSVMIPOVQAX-UHFFFAOYSA-N
InChI:
InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
Canonical SMILES:
C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F
1.β-Catenin inactivation is a pre-requisite for chick retina regeneration.
Zhu J;Luz-Madrigal A;Haynes T;Zavada J;Burke AK;Del Rio-Tsonis K PLoS One. 2014 Jul 8;9(7):e101748. doi: 10.1371/journal.pone.0101748. eCollection 2014.
In the present study we explored the role of β-catenin in mediating chick retina regeneration. The chick can regenerate its retina by activating stem/progenitor cells present in the ciliary margin (CM) of the eye or via transdifferentiation of the retinal pigmented epithelium (RPE). Both modes require fibroblast growth factor 2 (FGF2). We observed, by immunohistochemistry, dynamic changes of nuclear β-catenin in the CM and RPE after injury (retinectomy). β-Catenin nuclear accumulation was transiently lost in cells of the CM in response to injury alone, while the loss of nuclear β-catenin was maintained as long as FGF2 was present. However, nuclear β-catenin positive cells remained in the RPE in response to injury and were BrdU-/p27+, suggesting that nuclear β-catenin prevents those cells from entering the cell cycle. If FGF2 is present, the RPE undergoes dedifferentiation and proliferation concomitant with loss of nuclear β-catenin. Moreover, retinectomy followed by disruption of active β-catenin by using a signaling inhibitor (XAV939) or over-expressing a dominant negative form of Lef-1 induces regeneration from both the CM and RPE in the absence of FGF2. Our results imply that β-catenin protects cells of the CM and RPE from entering the cell cycle in the developing eye, and specifically for the RPE during injury.
2.The natural product 4,10-aromadendranediol induces neuritogenesis in neuronal cells in vitro through activation of the ERK pathway.
Chang S;Ruan WC;Xu YZ;Wang YJ;Pang J;Zhang LY;Liao H;Pang T Acta Pharmacol Sin. 2017 Jan;38(1):29-40. doi: 10.1038/aps.2016.115. Epub 2016 Nov 14.
Recent studies focus on promoting neurite outgrowth to remodel the central nervous network after brain injury. Currently, however, there are few drugs treating brain diseases in the clinic by enhancing neurite outgrowth. In this study, we established an NGF-induced PC12 differentiation model to screen novel compounds that have the potential to induce neuronal differentiation, and further characterized 4,10-Aromadendranediol (ARDD) isolated from the dried twigs of the Baccharis gaudichaudiana plant, which exhibited the capability of promoting neurite outgrowth in neuronal cells in vitro. ARDD (1, 10 μmol/L) significantly enhanced neurite outgrowth in NGF-treated PC12 cells and N1E115 cells in a time-dependent manner. In cultured primary cortical neurons, ARDD (5, 10 μmol/L) not only significantly increased neurite outgrowth but also increased the number of neurites on the soma and the number of bifurcations. Further analyses showed that ARDD (10 μmol/L) significantly increased the phosphorylation of ERK1/2 and the downstream GSK-3β, subsequently induced β-catenin expression and up-regulated the gene expression of the Wnt ligands Fzd1 and Wnt3a in neuronal cells. The neurite outgrowth-promoting effect of ARDD in neuronal cells was abolished by pretreatment with the specific ERK1/2 inhibitor PD98059, but was partially reversed by XAV939, an inhibitor of the Wnt/β-catenin pathway.
3.Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via β-catenin stabilization.
Jansen SR;Holman R;Hedemann I;Frankes E;Elzinga CR;Timens W;Gosens R;de Bont ES;Schmidt M J Cell Mol Med. 2015 Jan;19(1):210-26. doi: 10.1111/jcmm.12418. Epub 2014 Sep 30.
Amplification of MYCN is the most well-known prognostic marker of neuroblastoma risk classification, but still is only observed in 25% of cases. Recent evidence points to the cyclic adenosine monophosphate (cAMP) elevating ligand prostaglandin E2 (PGE2 ) and β-catenin as two novel players in neuroblastoma. Here, we aimed to define the potential role of PGE2 and cAMP and its potential interplay with β-catenin, both of which may converge on neuroblastoma cell behaviour. Gain and loss of β-catenin function, PGE2 , the adenylyl cyclase activator forskolin and pharmacological inhibition of cyclooxygenase-2 (COX-2) were studied in two human neuroblastoma cell lines without MYCN amplification. Our findings show that PGE2 enhanced cell viability through the EP4 receptor and cAMP elevation, whereas COX-2 inhibitors attenuated cell viability. Interestingly, PGE2 and forskolin promoted glycogen synthase kinase 3β inhibition, β-catenin phosphorylation at the protein kinase A target residue ser675, β-catenin nuclear translocation and TCF-dependent gene transcription. Ectopic expression of a degradation-resistant β-catenin mutant enhances neuroblastoma cell viability and inhibition of β-catenin with XAV939 prevented PGE2 -induced cell viability.
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