XAV-939 |
| Catalog No.GC12781 |
XAV-939 selectively inhibits β-catenin-mediated transcription.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 284028-89-3
Sample solution is provided at 25 µL, 10mM.
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XAV-939 selectively inhibits β-catenin-mediated transcription. XAV-939 stimulates β-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV939 stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2 with IC50 values of 5 nM and 2 nM, respectively [1，2].
XAV-939 inhibited mouse neurofibroma sphere formation with IC50 of 0.1 µM. Western blot confirmed a 50% decrease in total β-catenin with 3 days of XAV-939 exposure (10 nM) [3]. TNKS1 plays a role in cell cycle regulation and that XAV-939 induces an accumulation of NB cell lines at G2/M and S phase of the cell cycle [4].
XAV-939 increases Irradiation (IR) sensitivity of cervical cancer with the PIK3CA-E545K mutation in vivo, XAV-939 and IR inhibited tumor weight by 38% from IR alone in that with PIK3CA-WT [5]. Combinatorial inhibition of transforming growth factor-β (TGF-β) and WNT signaling with SB431542 and XAV-939 potently enhances the efficiency, quality, and speed of reprogrammed iCMs generated upon delivery of the minimal transcription factor (TF) cocktail, GMT, into postnatal cardiac fibroblasts. SB431542 and XAV-939 significantly improved in vivo reprogramming and cardiac function in mice compared with GMT alone and reduced the number of TFs needed for human reprogramming [6].
References:
[1]. S.M. Huang, Y.M. Mishina, S. Liu, A. Cheung, F. Stegmeier, G.A. Michaud, O. Charlat, E. Wiellette, Y. Zhang, S. Wiessner, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling.Nature, 461 (2009), pp. 614-620
[2]. Mohit Narwal, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9.
[3]. Wu J, Keng VW, Patmore DM, et al. Insertional mutagenesis identifies a STAT3/Arid1b/beta-catenin pathway driving neurofibroma initiation. Cell Rep. 2016;14:1979-90.
[4]. X.H. Tian, W.J. Hou, Y. Fang, J. Fan, H. Tong, S.L. Bai, et al. XAV939, a tankyrase 1 inhibitior, promotes cell apoptosis in neuroblastoma cell lines by inhibiting Wnt/β-catenin signaling pathway. J Exp Clin Cancer Res, 32 (1) (2013 Dec 5), p. 1
[5]. Jiang W, Wu Y, He T, et al. Targeting of beta-catenin reverses radioresistance of cervical cancer with the PIK3CA E545K mutation. Mol Cancer Ther 2020;19(2):337-47.
[6]. Mohamed, T. M. et al. Chemical enhancement of in vitro and in vivo direct cardiac reprogramming. Circulation 135, 978-995 (2017).
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells in the logarithmic growth phase were seeded in 96-well plates, at a density of 2×104 cells/well, and subsequently treated with various XAV-939 concentrations (0.1, 0.5, 1, 5, 10 µmol/l) for 24, 48, 72 and 96 h. |
Reaction Conditions | 0.1, 0.5, 1, 5, 10 µmol/l for 24, 48, 72 and 96 h |
Applications | At all experimental time points, XAV-939 treatment was able to significantly inhibit A549 cell proliferation compared with the control group (F24h=30.382, F48h=52.463, F72h=56.635, F96h=59.274), with the exception of the 5-and 10-µmol/l groups at the 24 h time point. |
| Animal experiment [2]: | |
Animal models | DBA/2 inbred mice |
Preparation Method | Mice received an intraperitoneal injection of 100 µl of XAV-939 (2 mg/ml) along with a 10% dimethyl sulfoxide (DMSO; compounded by 0.9% NaCl solution) every day since they received vaccination with the L1210 cells, while according to other experimental groups, mice received intraperitoneal injections along with 100 µl of 10% DMSO solution (compounded by 0.9% NaCl solution) for 21 days continuously. |
Dosage form | Intraperitoneal injection, 100 µl of 2 mg/ml for 21 days |
Applications | In the model, NC, HOTAIR mimics, siRNA HOTAIR, XAV-939, and HOTAIR mimics + XAV-939 groups, the WBC number in PB increased on the 21st day by 341.08, 355.72, 499.85, 196.49, 187.48, and 363.35%. However, the PLT number decreased by 66.37, 69.46, 81.27, 49.24, 50.47, and 72.61%; hemoglobin content decreased by 39.02, 41.05, 60.52, 14.01, 17.20, and 42.36%. |
References: | |
| Cas No. | 284028-89-3 | SDF | |
| Chemical Name | 2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one | ||
| Canonical SMILES | C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F | ||
| Formula | C14H11F3N2OS | M.Wt | 312.31 |
| Solubility | ≥ 15.62mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2019 mL | 16.0097 mL | 32.0195 mL |
| 5 mM | 0.6404 mL | 3.2019 mL | 6.4039 mL |
| 10 mM | 0.3202 mL | 1.601 mL | 3.2019 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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