k-ras-in-1

Description: K-Ras-IN-1 (formerly known as K-Ras-Inhibitor-1) is a novel small molecule K-Ras inhibitor that binds to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure, in other words, K-Ras-IN-1 binds directly to K-Ras between switch I and switch II and inhibit Sos-catalyzed K-Ras activation. By binding to K-Ras and blocking the binding to Sos, it causes the inhibition of Sos-mediated nucleotide exchange. K-Ras-IN-1 represents a starting point for obtaining probe molecules useful in elucidating new insights into Ras signaling and for discovering K-Ras inhibitors for the treatment of cancer.

References: J Chem Inf Model. 2014 Feb 24; 54(2):530-8; Angew Chem Int Ed Engl. 2012 Jun 18; 51(25):6140-3.