2C07

2C07 is a mutant Ras (K-Ras^M72C, H-Ras^M72C) inhibitor. 2C07 blocks the activation of PI3K through allosteric Ras modification. 2C07 binds to the modified switch II pocket (S-IIG) of Ras in both GDP- and GTP-bound states, stabilizes the GDP-bound state, disrupts the polar interactions of the canonical GTP-bound state, and inhibits SOS binding and nucleotide exchange. 2C07 can be used in cancer-related research^[1]. In Vitro:2C07 selectively binds to the engineered Cys72 residue in truncated K-Ras^M72C GDP and truncated H-Ras^M72C GppNHp with βME₅₀ values of 2.53 mM and 1.10 mM, respectively, and does not modify wild-type Ras constructs^[1].
2C07 binds to the switch-II groove (S-IIG) of truncated K-Ras^M72C GDP and truncated H-Ras^M72C in both GDP and GppNHp states, inducing a modified switch-II pocket conformation and, in the GppNHp state, altering switch I positioning and Mg²⁺ coordination^[1].