KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
KRpep-2d binds to K-Ras（G12D）with a Kd of 8.9 nM and approximately 6-fold selectivity over WT K-Ras, leading to an extended dissociation half-life[1]. KRpep-2d significantly suppresses ERK-phosphorylation, downstream of K-Ras(G12D), along with A427 cancer cell proliferation at 30 μM peptide concentration[2].
[1] Satoshi Sogabe, et al. ACS Med Chem Lett. 2017, 8:732?736. [2] Sakamoto K, et al. Biochem Biophys Res Commun. 2017 Mar 11, 484(3):605-611.