ArtNr |
S1180-5000 |
Hersteller |
Selleckchem
|
CAS-Nr. |
284028-89-3 |
Menge |
5 g |
Kategorie |
|
Typ |
Inhibitors |
Specific against |
other |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Alias |
NVP-XAV939, TNKS1, TNKS2;Wnt/beta-catenin |
Similar products |
XAV-939 |
Lieferbar |
|
Cell lines |
WTK1 lymphoblasts |
Chemical Name |
2-(4-(trifluoromethyl)phenyl)-7, 8-dihydro-5H-thiopyrano[4, 3-d]pyrimidin-4-ol |
Concentrations |
1.0 uM |
Description |
XAV-939 is a selective Wnt beta-catenin-mediated transcription inhibitor for TNKS1 and TNKS2 with IC50 of 11 nM and 4 nM, respectively. |
IC50 |
11 nM, 11 nM, 11 nM, 11 nM, 11 nM, 11 nM |
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 uM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 uM 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] |
Incubation Time |
8 hours |
Method |
XAV-939 is solubilized in DMSO at 55 C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 uM. WTK1 lymphoblasts treated with either DMSO or 1.0 uM XAV-939 for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and XAV-939 samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls. |
Molecular Weight (MW) |
312, 31 |
Picture ChemicalStructure Description |
XAV-939 Chemical Structure |
Picture Description 1 |
, , Dr Marco Quarta of Stanford University, XAV-939purchased from Selleck, Cells plated at 2 x 104 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment without wnt) switch medium from 2% HS + WNT 100 ng/ml |
Solubility (25C) |
DMSO 15 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL |
Storage |
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO |
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