SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor that 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. It is intended for research use only.
- Binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, Q61H) with nanomolar affinity
- Directly blocks nucleotide association
- Impairs KRAS-driven cancer cell viability
- Blocks ERK-MAPK phosphosignaling cascade downstream of KRAS
- Exhibits IC50 values in 5-15 μM range for cancer cells with KRAS mutations
- Inhibits MEK1/2, ERK1/2, and AKT phosphorylation in vitro