SHOC2–RAS PPI-IN-1

SHOC2–RAS PPI-IN-1 (compound 6) is a non-covalent competitive inhibitor that targets the interaction between SHOC2 and RAS proteins. It exhibits an IC50 of 0.048 μM and a KD of 0.065 μM against NRASQ61R. This compound inhibits SMP phosphatase-complex activity, increasing CRAFS259 phosphorylation levels and thus blocking the MAPK signaling pathway (by reducing pMEK and pERK levels) . It induces cell cycle arrest and apoptosis in tumor cells. SHOC2–RAS PPI-IN-1 is used in targeting studies for malignancies, such as NRASQ61R-mutant melanoma and colorectal cancer.