Description

WAY-316606 is an inhibitor of secreted frizzled-related protein 1 (sFRP-1; IC₅₀ = 0.5 μM). It increases Wnt signaling in U2OS osteosarcoma cells (EC₅₀ = 0.65 μM). WAY-316606 increases total bone area in a murine calvarial organ culture assay when used at concentrations greater than 0.1 nM.

Uses

WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM[1].

Definition

ChEBI: WAY-316606 is a sulfonamide resulting from the formal condensation of the sulfonic acid group of 5-(phenylsulfonyl)-2-(trifluoromethyl)benzenesulfonic acid with the primary amino group of piperidin-4-amine. An inhibitor of secreted Frizzled-Related Protein-1 (sFRP-1). It has a role as a secreted frizzled-related protein 1 inhibitor. It is a sulfone, a sulfonamide, a member of (trifluoromethyl)benzenes, a member of piperidines and a secondary amino compound.

in vivo

References

[1] Moore, WJ, et al. Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides. Journal of Medicinal Chemistry (2009), 52(1), 105-116. DOI:10.1021/jm801144h
[2] Bodine PV, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone. 2009 Jun;44(6):1063-8. DOI:10.1016/j.bone.2009.02.013