Antibodies
XAV-939
- 貨號 Cat. No.
- S1180
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
XAV-939
XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM, regulates axin levels and does not affect CRE, NF-κB or TGF-β. | |||||
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| Targets | TNKS1 | TNKS2 | ||||
| IC50 | 11 nM | 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] | |||||
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| Features | ||||||
Protocol(Only for Reference)
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. |
References
Chemical Information
| Molecular Weight (MW) | 312.31 |
|---|---|
| Formula | C14H11F3N2OS |
| CAS No. | 284028-89-3 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 12 mg/mL (38 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.31231 | 3.1231 | 6.2462 | 9.3693 |
Customer Reviews (3)
 Click to enlarge | Rating | |
| Source | XAV-939 purchased from Selleck | |
| Method | Sectional Immunohistochemistry | |
| Cell Lines | E14.5 male UGSs | |
| Concentrations | 10 μM | |
| Incubation Time | 4 d | |
| Results | Total bud numbers were compared among vehicle9 (control), TCDD9 (1 nM), DKK1 + DKK29 (500 ng/ml each), and XAV-939-(10 μM) treated UGSs by staining the UGE for e-cadherin and counting prostatic buds. All treatments decreased the total number of prostatic buds compared to control UGSs (p<0.05, Fig. 1, bottom). A confocal image that is representative of the UGS for each treatment is also shown (Fig. 1, top). |
Product Citations (9)
In vivo transcriptional governance of hair follicle stem cells by canonical Wnt regulators. [Lien WH, et al. Nat Cell Biol 2014;16(2):179-90]
Synergistic Activities of MET/RON Inhibitor BMS-777607 and mTOR Inhibitor AZD8055 to Polyploid Cells Derived from Pancreatic Cancer and Cancer Stem Cells. [Zeng JY, et al. Mol Cancer Ther 2013;13(1):37-48]
Tbx20 promotes cardiomyocyte proliferation and persistence of fetal characteristics in adult mouse hearts. [Chakraborty S, et al. J Mol Cell Cardiol 2013;62:203-13]
