KS-58

KS-58 is a **first-in-class, selective bicyclic peptide inhibitor** that targets the K-Ras(G12D) mutant protein. It binds both the GDP- and GTP-bound forms of K-Ras(G12D) with high affinity (Ki = 22 nM) and inhibits the interaction of K-Ras(G12D) with downstream effector proteins, disrupting Ras/ERK signaling and suppressing cancer cell proliferation. KS-58 demonstrates selective cytotoxicity against cell lines and animal xenografts expressing K-Ras(G12D), including human lung (A427) and pancreatic (PANC-1) cancer cells, with significantly reduced effectiveness in non-G12D Ras mutants. The peptide is delivered experimentally via intravenous injection and has shown reasonable safety and anti-tumor activity in preclinical models. KS-58 was generated and chemically synthesized using Fmoc-based solid-phase peptide synthesis technology[3][5][6].

Brand names

KS-58KS58KS 58

Other names

KS-58KS58KS 58