WAY-262611

WAY-262611 is a small molecule agonist of the Wnt/β-catenin signaling pathway that acts by inhibiting Dickkopf-1 (DKK1). DKK1 is a secreted Wnt antagonist that binds to LRP5/6 co-receptors and Kremen, leading to LRP5/6 internalization and pathway suppression. By blocking the formation of the DKK1-LRP5/6-Kremen complex, WAY-262611 prevents LRP5/6 internalization, thereby restoring Wnt/β-catenin signaling. Originally developed by Wyeth Research for the treatment of osteoporosis, WAY-262611 has demonstrated the ability to increase the bone formation rate in vivo. Additionally, preclinical studies have explored its potential in oncology, including hepatocellular carcinoma and alveolar rhabdomyosarcoma, where DKK1 inhibition can suppress tumor progression and modulate the immune microenvironment.

Other names

(1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamineBML-WN110BML-WN-110BML-WN 110Dickkopf-1 InhibitorDickkopf1 InhibitorDickkopf 1 InhibitorWAY-262611 dihydrochlorideWAY262611 dihydrochlorideWAY 262611 dihydrochlorideWAY-262611 hydrochlorideWAY262611 hydrochlorideWAY 262611 hydrochlorideWnt Pathway Activator VI