Deltarasin

Description: Deltarasin (also known as Deltarasin hydrochloride) is a novel, high affinity and potent small molecule inhibitor of KRAS-PDEdelta protein-protein interaction with potential antineoplastic activity. It inhibits KRAS-PDEdelta interaction with a Kd of 38 nM for binding to purified PDEdelta. The KRAS oncogene product is considered a major target in anticancer drug discovery. 5 mM of deltarasin completely inhibited PDEdelta-KRAS interaction and released the insolubilized mCitrine-RHEB/KRAS6Q to the endomembrane system. This showed that deltarasin interfered with the binding of KRAS to PDEdelta in cells and thereby inhibited its solubilization

References: Nature. 2013 May 30; 497(7451):638-42.

Related CAS: 1440898-61-2 (free base); 1440898-82-7 (HCl)

Chemical Name: 2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole, trihydrochloride

InChi Key: NCIOVAYUMQEQEU-VKZSUDIWSA-N

InChi Code: InChI=1S/C40H37N5O.3ClH/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31; ; ; /h1-22, 30, 38, 41H, 23-28H2; 3*1H/t38-; ; ; /m1.../s1