KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Displays cytotoxicity in KRas-driven cancer cell lines and inhibits downstream ERK-MAPK signaling. Cell permeable.
Leshchiner et al (2015) Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc.Natl.Acad.Sci.USA. 112 1761 PMID:25624485