N-Ras Inhibitor

RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (K_d = 195 nM) and KRAS (G12V) (K_d = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS^G12C cancer models, and demonstrates good tolerability across various RAS cancer models.

SHOC2-RAS PPI-IN-1 is a SHOC2-NRAS interaction inhibitor with IC₅₀ of 0.048 μM and a K_d of 0.065 μM for SHOC2. SHOC2-RAS PPI-IN-1 inhibits RAS/MAPK signalling and downregulates MEK and ERK phosphorylation. SHOC2-RAS PPI-IN-1 can inhibit cells proliferation in RAS-mutant cancer models. SHOC2-RAS PPI-IN-1 can be used for the research of RAS-mutant cancers.

Anticancer agent 207 (compound 10b) is a potent anticancer agent. Anticancer agent 207 bounds to the NRAS rG4 with a K_D value of 2.31 µM. Anticancer agent 207 shows cytotoxicity and decreases the expression of NRAS protein. Anticancer agent 207 shows antitumor activity.