Research Area
Product Type
United States ( Change Country )
XAV-939 Chemical Structure
Recommended Products
ICG-001
ICG-001 is a selective Wnt/β-catenin signalling inhibitor with an IC50 of 3μM.
GDC-0449 (Vismodegib)
GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM.
Cyclopamine
Cyclopamine is a Smo or hedgehog signaling pathway inhibitor.
DAPT (GSI-IX)
DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 of 0.12 and 0.2 μM for total Aβ and Aβ42 levels, respectively.
LY2940680
LY2940680 is a potent agent used to treat cancer.
ICG-001
ICG-001 is a selective Wnt/β-catenin signalling inhibitor with an IC50 of 3μM.
LY-411575
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor with an IC50 of 0.1 nM for APP23 and APP51/16 primary neurons.
Biological Activity
| Information | XAV-939 is a small molecule and selective Wnt pathway transcription factor β-catenin-mediated transcription inhibitor to TNKS1 and TNKS2 with IC50 of 11 nM and 4 nM, respectively. | |||||
|---|---|---|---|---|---|---|
| Targets | TNKS1 | TNKS2 | ||||
| IC50 | 11 nM [1] | 4 nM [1] | ||||
| 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] | |||||
| In vivo | ||||||
| Clinical Trials | ||||||
| Features | ||||||
Protocol
Cell Assay: [1]
| Cell lines: | WTK1 lymphoblasts |
|---|---|
| Concentrations: | 1.0 μM |
| 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 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM 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. |
Chemical Information
| Molecular Weight (WM): | 312.31 |
|---|---|
| Formula: | C14H11F3N2OS |
| CAS No.: | 284028-89-3 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥3mg/mL |
| Water <1mg/mL | |
| Ethanol ≥5mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
Related Inhibitors
Recommended Screening Libraries
Chemical Library
A collection of 864 bioactive compounds
Inhibitor Library
A collection of 481 inhibitors
Kinase Inhibitor Library
A collection of 194 kinase inhibitors
Tyrosine Kinase Inhibitor Library
A collection of 85 tyrosine kinase inhibitors.
FDA Approved Drug Library
A collection of 426 FDA approved drugs
Natural Product Library
A collection of 139 natural products
Chemotherapeutic Agent Library
A collection of 40 chemotherapeutic agents
Epigenetics Compound library
A unique collection of 17 small molecule modulators
Stem Cell Compound library
A unique collection of 47 small molecule inhibitors
GPCR Compound library
A unique collection of 63 GPCR small molecules
Selleck's high quality products have been used in several published research findings, including the following:
Ribosomal Protein S6 Kinase (RSK)-2 as a central effector molecule in RON receptor tyrosine kinase mediated epithelial to mesenchymal transition induced by macrophage-stimulating protein
We have 1 customer reviews of XAV-939.
- (0)
- (1)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
Average Customer Review
(1 customer reviews)
-
Click to enlarge
cells plated at 2 x 10E4 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment withour wnt) switch medium from 2% HS + WNT 100 ng/ml
cells plated at 2 x 10E4 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment withour wnt) switch medium from 2% HS + WNT 100 ng/ml
Data independently produced by Dr Marco Quarta of Stanford University XAV-939 purchased from Selleck
This product has been referenced in
Check our customer reviews
cells plated at 2 x 10E4 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment withour wnt) switch medium from 2% HS + WNT 100 ng/ml |
Data independently produced by Dr Marco Quarta of Stanford University
We give free samples and rewards to people who would like to provide us useful scientific data(western blot, etc.) > See Details
Recently Viewed Items
Keywords:buy XAV-939 | XAV-939 supplier | purchase XAV-939 | XAV-939 cost | XAV-939 manufacturer | order XAV-939 | XAV-939 distributor