A potent TNKS1/2 inhibitor
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WIKI4

Item No. 14057

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[3-[[4-(4-methoxyphenyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]propyl]-1H-benz[de]isoquinoline-1,3(2H)-dione
CAS Number
838818-26-1
Synonyms
  • Tankyrase 1/2 Inhibitor V
Molecular Formula
C29H23N5O3S
Formula Weight
521.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:5): 0.1 mg/mlDMSO: 2 mg/ml
λmax
232, 279, 332, 343 nm
SMILES
O=C(C1=C2C3=CC=CC2=CC=C1)N(CCCSC4=NN=C(C5=CC=NC=C5)N4C6=CC=C(OC)C=C6)C3=O
InChi Code
InChI=1S/C29H23N5O3S/c1-37-22-11-9-21(10-12-22)34-26(20-13-15-30-16-14-20)31-32-29(34)38-18-4-17-33-27(35)23-7-2-5-19-6-3-8-24(25(19)23)28(33)36/h2-3,5-16H,4,17-18H2,1H3
InChi Key
RNUXIZKXJOGYQP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    WIKI4 is a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively).1,2 It has little or no effect on related polymerases or transferases at 10 µM.2 Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway.1 WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. James, R.G., Davidson, K.C., Bosch, K.A., et al. WIKI4, a novel inhibitor of tankyrase and Wnt/β-catenin signaling. PLoS One 7(12), 1-10 (2012).

    2. Haikarainen, T., Venkannagari, H., Narwal, M., et al. Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4. PLoS One 8(6), 1-8 (2013).