A Dkk1 inhibitor and Wnt signaling activator
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WAY-262611

Item No. 17704

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-(2-naphthalenyl)-2-pyrimidinyl]-4-piperidinemethanamine
CAS Number
1123231-07-1
Synonyms
  • BML-WN110
  • Dickkopf-1 Inhibitor
  • Dkk1 Inhibitor
Molecular Formula
C20H22N4
Formula Weight
318.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 50 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
226, 256, 338 nm
SMILES
NCC1CCN(C2=NC(C3=CC(C=CC=C4)=C4C=C3)=CC=N2)CC1
InChi Code
InChI=1S/C20H22N4/c21-14-15-8-11-24(12-9-15)20-22-10-7-19(23-20)18-6-5-16-3-1-2-4-17(16)13-18/h1-7,10,13,15H,8-9,11-12,14,21H2
InChi Key
QHLITPHIARVDJI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.1,2,3 Dickkopf-1 (Dkk1) antagonizes Wnt signaling and has important roles in bone formation, cancer, and Alzheimer’s disease.4 WAY-262611 is an inhibitor of Dkk1 that activates the Wnt signaling pathway, stimulating β-catenin/TCF-dependent transcription with an EC50 value of 0.63 µM.5 It has good pharmacokinetic properties and increases trabecular bone formation in ovariectomized rats following oral administration.5 WAY-262611 has been used to elucidate the role of Dkk1 in modulating Wnt signaling, particularly in the context of arthritis.6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Polakis, P. Wnt signaling and cancer. Genes Dev. 14(15), 1837-1851 (2000).

    2. Reya, T., and Clevers, H. Wnt signalling in stem cells and cancer. Nature 434(7035), 834-850 (2005).

    3. Clevers, H. Wnt/β-catenin signaling in development and disease. Cell 127(3), 469-480 (2006).

    4. Hameed, A., Brady, J.J., Dowling, P., et al. Bone disease in multiple myeloma: pathophysiology and management. Cancer Growth Metastasis 7, 33-42 (2014).

    5. Pelletier, J.C., Lundquist, J.T.t., Gilbert, A.M., et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a winglessβcatenin agonist that increases bone formation rate. J. Med. Chem. 52(22), 6962-6965 (2009).

    6. Enochson, L., Stenberg, J., Brittberg, M., et al. GDF5 reduces MMP13 expression in human chondrocytes via DKK1 mediated canonical Wnt signaling inhibition. Osteoarthritis Cartilage 22(4), 566-577 (2014).

    7. Choe, Y., Hun Kim, J., Park, K.Y., et al. Activation of dickkopf-1 and focal adhesion kinase pathway by tumour necrosis factor α induces enhanced migration of fibroblast-like synoviocytes in rheumatoid arthritis. Rheumatology (Oxford) 55(5), 928-938 (2015).