UP-6

UP-6 is a small molecule inhibitor of the actin-binding protein profilin-1 (Pfn1), specifically designed to disrupt the Pfn1-actin interaction. It is a trifluoromethyl structural analog of a previously identified brominated lead compound, optimized for enhanced anti-angiogenic activity. In clear cell renal cell carcinoma (RCC), Pfn1 is overexpressed in tumor-associated vascular endothelial cells and plays a critical role in promoting angiogenesis and tumor growth. UP-6 binds directly to Pfn1, thereby attenuating the formation of new blood vessels within the tumor microenvironment. Research has also explored the use of lipid microbubble encapsulation for UP-6, enabling targeted delivery and ultrasound-triggered release to maximize therapeutic benefit while minimizing systemic effects.

Other names

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