Frizzled-4 inhibitors comprise a class of chemicals that either directly or indirectly modulate the activity of the frizzled-4 receptor. While there are no direct inhibitors identified, several compounds target key components of the Wnt signaling pathway to impact frizzled-4 indirectly. LGK-974 and IWP-2 act as porcupine inhibitors, indirectly influencing frizzled-4 by disrupting Wnt ligand secretion. KY02111 interferes with Wnt/β-catenin signaling by blocking the interaction between β-catenin and TCF/LEF transcription factors, downregulating frizzled-4 activity. NSC 668036 and XAV939 are tankyrase inhibitors that indirectly impact frizzled-4 by modulating the canonical Wnt pathway. PRI-724 is a CBP/β-catenin inhibitor that indirectly influences frizzled-4 by disrupting the interaction between β-catenin and CBP, inhibiting Wnt/β-catenin signaling.
PKF115-584 and C59, both tankyrase inhibitors, regulate frizzled-4 through the Wnt/β-catenin pathway. They stabilize Axin, promoting the degradation of β-catenin, leading to inhibition of Wnt signaling and influencing frizzled-4 activation. Wnt-C59, another porcupine inhibitor, targets Wnt ligand secretion, impacting frizzled-4 through disruption of the canonical Wnt pathway. IWR-1-endo and G007-LK, tankyrase inhibitors, modulate frizzled-4 by affecting the Wnt/β-catenin pathway. They stabilize Axin, leading to increased degradation of β-catenin and inhibition of Wnt signaling, thereby influencing frizzled-4 activation. FH535 is a Wnt/β-catenin signaling inhibitor that suppresses β-catenin interaction with transcription factors, downregulating frizzled-4 activity. In summary, these frizzled-4 inhibitors provide valuable tools for researchers to dissect the intricacies of Wnt signaling and its impact on frizzled-4 receptor activation. Understanding the specific pathways influenced by each inhibitor is crucial for unraveling the complexities of frizzled-4 modulation and its implications in cellular processes.