k-ras-inhibitor-6

Description: K-Ras (G12C) inhibitor 6 is a novel, potent, allosteric/irreversible, cysteine-reactive small molecule and selective inhibitor of oncogenic K-Ras(G12C) that causes 100% modification of the protein when used at 10 uM for 24 hours in vitro. It binds to the G12C mutantion of GTPase K-Ras irreversibly but does not bind the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras.

References: Nature. 2013 Nov 28; 503(7477):548-51.