C74

C74 is a small molecule inhibitor of the actin-binding protein profilin-1 (Pfn1), specifically designed to disrupt the Pfn1-actin interaction. It is a structural analog of an earlier inhibitor (often designated as C1), optimized with a trifluoromethyl group to enhance anti-angiogenic potency. Profilin-1 is frequently overexpressed in the vascular endothelial cells of clear cell renal cell carcinoma (RCC), where it promotes tumor angiogenesis and progression. C74 binds directly to Pfn1, attenuating the migration of endothelial cells and reducing tumor vascularization. Preclinical research has explored its delivery via lipid microbubble encapsulation, which allows for localized release in the tumor microenvironment through ultrasound-mediated disruption, thereby minimizing systemic effects while maximizing anti-tumor benefit in RCC models.

Other names

4,4'-((4-(trifluoromethyl)phenyl)methylene)bis(3,5-dimethyl-1H-pyrazole)