Item no. |
S1180-5000 |
Manufacturer |
Selleckchem
|
CASRN |
284028-89-3 |
Amount |
5 g |
Category |
|
Type |
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 |
Available |
|
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 |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.