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XAV-939Tankyrase 1/2 inhibitor

XAV-939

Catalog No. A1877
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
Evaluation Sample $28.00 In stock
5mg $50.00 In stock
25mg $120.00 In stock
100mg $300.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

XAV-939

Related Biological Data

XAV-939

Related Biological Data

XAV-939

Biological Activity

XAV-939 is a inhibitor of TNKS1 and TNKS2 with IC50 of 11 and 4 nM, respectively.
Targets TNKS1 TNKS2        
IC50 11 nM 4 nM        

Protocol

Cell experiment: [1]

Cell lines

HCT116 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

20 μM, 24 hours

Applications

HCT116 cells were treated with XAV-939, then stained with PI and subjected to flow cytometric analysis or lysed and subjected to immunoblot analysis. The results showed that the number of cells arrest in G1 phase was 71.01%, as compared with the 45.54% of untreated control samples. Western blot analysis revealed that XAV-939 increased the level of AXIN and inhibited the expression of β-catenin.

Animal experiment: [2]

Animal models

Mice

Dosage form

Intraperitoneal injection, 2.5 mg/kg, four times a day

Applications

Treatment of bleomycin challenged mice with XAV-939 reduced dermal thickening by 50% compared with sham-treated, bleomycin challenged mice. The number of myofibroblasts and the hydroxyproline content were also significantly decreased in mice treated with XAV-939.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] He L, Lu N, Dai Q, et al. Wogonin induced G1 cell cycle arrest by regulating Wnt/β-catenin signaling pathway and inactivating CDK8 in human colorectal cancer carcinoma cells. Toxicology, 2013, 312: 36-47.

[2] Distler A, Deloch L, Huang J, et al. Inactivation of tankyrases reduces experimental fibrosis by inhibiting canonical Wnt signalling. Annals of the rheumatic diseases, 2013, 72(9): 1575-1580.

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Chemical Properties

Cas No. 284028-89-3 SDF Download 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 >15.6mg/mL in DMSO Storage Store at -20°C
General tips No
Shipping Condition No

Background

XAV-939 is a small-molecule inhibitor of tankyrase 1/2 with IC50 values of 4 and 11 nM, respectively [1].

XAV-939 was screened out as an inhibitor of Wnt/β-catenin pathway. In HEK293 cells, XAV-939 significantly inhibited the Wnt3a-stimulated STF activity and β-catenin accumulation. In SW480 cells, XAV-939 also inhibited STF activity and increased β-catenin phosphorylation. XAV-939 was demonstrated to stabilize the axin levels through inhibiting tankyrases and subsequently inhibit the Wnt signaling. It tightly bound to the catalytic domains of tankyrase 1 and tankyrase 2 with Kd values of 99 and 93 nM, respectively. In addition, XAV-939 significantly inhibited colony formation of β-catenin-dependent DLD-1 cells but not β-catenin-independent RKO cells [1].

References:
[1] Huang S M A, Mishina Y M, Liu S, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature, 2009, 461(7264): 614-620.