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.
The Wnt signaling pathway is activated by secreted Wnt glycoproteins and regulates various biological processes, including skeletal development. Secreted frizzled-related protein-1 (sFRP-1) is a negative regulator or an antagonist of the Wnt signaling pathway. WAY-316606 is identified as an inhibitor of sFRP-1 with IC50 value of 0.5 μM[3]. WAY-316606 enhanced total bone area up to 60% in a dose-dependent manner when tested in a neonatal murine ex vivo calvarial assay[3]. WAY-316606 treated rat mandibles (1 mM, 10 uL, on alternate days for 7 days) showed a substantial gain of interradicular bone mass near the inhibitor application site compared to rat mandibles treated with a vehicle control, in MicroCT analysis[4]. Differentiating periodontal ligament cells cultured with 1 and 2 uM of WAY-316606 showed increased alkaline phosphatase activity and enhanced mineral deposits in a dose dependent manner compared to cells cultured with induction media alone[4].
作用机制
WAY-316606 inhibits sFRP-1 perhaps via the netrin domain.
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