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MC-1-F2 is a first-in-class small-molecule inhibitor of the transcription factor Forkhead box protein C2 (FOXC2). FOXC2 is a central mediator of the epithelial-mesenchymal transition (EMT), a process that allows cancer cells to acquire metastatic properties, cancer stem cell (CSC) phenotypes, and resistance to therapy. MC-1-F2 works by inducing the degradation of FOXC2 and blocking its nuclear localization, thereby reversing EMT and inhibiting cancer cell migration and invasion. It has been studied primarily in the context of castration-resistant prostate cancer (CRPC) and breast cancer, where it has shown potential to sensitize cells to chemotherapy agents like docetaxel.
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