lrp6

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, specifically inhibits the growth of gram-positive bacteria, acts as a potent inhibitor of Wnt β-catenin signaling by blocking Wnt-induced LRP6 phosphorylation, and demonstrates selective activity against human cancer stem cells.

IWP-O1, a highly potent Porcupine (Porcn) inhibitor (EC50: 80 pM), effectively suppresses the phosphorylation of Dvl2 3 and LRP6 in HeLa cells.

Gigantol is a novel inhibitor of the Wnt/β-catenin pathway. It inhibits Wnt/β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells. Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases, it shows the protective effect against hydrogen peroxide-induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K/Akt pathway.Gigantol inhibits aldose reductase gene to exert its anti-cataract activity. Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K/Akt/NF-κB signaling pathway.Gigantol also shows α-glucosidase inhibitory activity.

Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt β-catenin signaling.

Salinomycin sodium salt (Sodium salinomycin), an antibiotic potassium ionophore, is an effective inhibitor of Wnt β-catenin signaling.