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.
Target:
Apoptosis|||Ras
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