A TNKS inhibitor
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XAV939

Item No. 13596

Technical Information
Formal Name
3,5,7,8-tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
CAS Number
284028-89-3
Molecular Formula
C14H11F3N2OS
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:5): 0.15 mg/mlDMSO: 2 mg/ml
SMILES
OC1=NC(C2=CC=C(C(F)(F)F)C=C2)=NC3=C1CSCC3
InChi Code
InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
InChi Key
KLGQSVMIPOVQAX-UHFFFAOYSA-N
Origin
Synthetic
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively.1 By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells.1 At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.1 This product is also available as part of Cayman's Fibroblast Reprogramming Reagent Kit (SB/XAV) (Item No. 502888).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, S.M.A., Mishina, Y.M., Liu, S., et alTankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461, 614-619 (2009).