Potent and water soluble inhibitor of secreted Frizzled-Related Protein I (sFRP-1; Kd value 0.08 μM and EC50 value 0.65 μM for Wnt-luciferase activity from U2-OS cells) that stimulates the Wnt/β-catenin canonical signaling pathway. WAY316606 increased total bone area in a murine calvarial organ culture assay at concentrations as low as 0.0001 μM. WAY-316606 also bound to sFRP-2, albeit over 10 times weaker (Kd value 1.0 μM) and shows moderate to low inhibition of cytochrome p450 isozymes (3A4, 2D6, 2C9) and good stability in rat and human liver microsomes (t1/2 > 60 min in each species).