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Home   »   Product Pathways  »  PARP  »  XAV-939

Products are for research use only. Not for human use. We do not sell to patients.


CS-0494 XAV-939


(XAV939;NVP-XAV 939)
Structure Price and Availability of    XAV-939
United States
Size Price Stock
5mg $50 In-stock Inquiry
10mg $60 In-stock
50mg $180 In-stock
100mg $280 In-stock
200mg $500 In-stock
500 mg Get quote
1 g Get quote
 Distributor In Japan:  フナコシ株式会社 www.funakoshi.co.jp    電話番号:81-3-5684-1620   
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  • Data Sheet
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XAV-939  M.Wt:  312.31
XAV-939  Formula: C14H11F3N2OS
XAV-939  Solubility: DMSO:≥ 21.5 mg/mL
XAV-939  Purity: >98%
XAV-939  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 284028-89-3

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XAV939 is a small molecule and selective Wnt pathway β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 of 11 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively. IC50 Value: 11 nM(TNKS1); 4 nM(TNKS2) Target: TMKS1/2; β-catenin 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. 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. in vivo: N/A

PARP  |   β-catenin  |  
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