Description

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), 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[1].—Neuroscience-Neuromodulation–C100H159N27O28—-[1]Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.–1652561-87-9–2187.50—-O=C(N[C@H](C(NCC(N[C@@H]([C@@H](C)CC)C(N[C@](C(N[C@H](C(N[C@@](C(N[C@H](C1=O)CC(N)=O)=O)([H])[C@H](O)C)=O)CC(C)C)=O)(CCCC=CCCC[C@](C)(N1)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(NCC(N[C@H](C(O)=O)CC(N)=O)=O)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)CC2=CC=CC=C2)[C@@H](NC([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)=O)CC3=CC=CC=C3–Cancer–10 mM in DMSO–Ras–K-Ras–GPCR/G Protein;MAPK/ERK Pathway–Peptides