SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. It binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). This compound directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.
- Peptide-based SOS1/KRAS protein interaction inhibitor
- Binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, Q61H) with nanomolar affinity
- Directly and independently blocks nucleotide association
- Impairs cancer cell viability
- Inhibits MEK1/2, ERK1/2, and AKT phosphorylation