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Formula | C14H11F3N2OS |
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Molecular Weight | 312.31 | CAS No. | 284028-89-3 | ||||
Solubility (25°C)* | In vitro | DMSO | 12 mg/mL (38.42 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. | ||||
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In vitro | XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. [1] XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. [2] |
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In vivo | AV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition. |
Cell Assay: |
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Animal Study: |
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Data from [Data independently produced by Nat Commun, 2014, 5, 5455]
Data from [Data independently produced by Dis Model Mech, 2014, 7(10), 1193-203]
, , Cancer Lett, 2017, 400:194-202
, , Dr. Marco Quarta of Stanford University
Double-Network DNA Macroporous Hydrogel Enables Aptamer-Directed Cell Recruitment to Accelerate Bone Healing [ Adv Sci (Weinh), 2024, 11(1):e2303637] | PubMed: 37949678 |
Activation of the Wnt/β-catenin signalling pathway enhances exosome production by hucMSCs and improves their capability to promote diabetic wound healing [ J Nanobiotechnology, 2024, 22(1):373] | PubMed: 38926800 |
RNF166 promotes colorectal cancer progression by recognizing and destabilizing poly-ADP-ribosylated angiomotins [ Cell Death Dis, 2024, 15(3):211] | PubMed: 38480683 |
The chromodomain protein CDYL confers forebrain identity to human cortical organoids by inhibiting neuronatin [ Cell Rep, 2024, 43(10):114814] | PubMed: 39378153 |
Pten regulates endocytic trafficking of cell adhesion and Wnt signaling molecules to pattern the retina [ Cell Rep, 2024, 43(4):114005] | PubMed: 38551961 |
Extraembryonic mesoderm cells derived from human embryonic stem cells rely on Wnt pathway activation [ Cell Prolif, 2024, 10.1111/cpr.13761] | PubMed: 39385268 |
GPA33 expression in colorectal cancer can be induced by WNT inhibition and targeted by cellular therapy [ Oncogene, 2024, ] | PubMed: 39472498 |
Elucidation of the pluripotent potential of bovine embryonic lineages facilitates the establishment of formative stem cell lines [ Cell Mol Life Sci, 2024, 81(1):427] | PubMed: 39377807 |
Cpt1a Drives primed-to-naïve pluripotency transition through lipid remodeling [ Commun Biol, 2024, 7(1):1223] | PubMed: 39349670 |
Deficiencies in corin and atrial natriuretic peptide-mediated signaling impair endochondral ossification in bone development [ Commun Biol, 2024, 7(1):1380] | PubMed: 39443661 |
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