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XAV-939 Chemical Structure

XAV-939

Data Sheet For research use only. Not for human use.
Cat. No. :BCP02128CAS No. :284028-89-3Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 284028-89-3 Cat. No. BCP02128
Name XAV-939
Synonyms XAV939;XAV 939;NVP-XAV 939;
SMILES
Chemical Name
Formula C14H11F3N2OS M. Wt 312.31
Purity 98% Storage Store at 4-8°C
Description 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.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.
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