EHop-016 at (LY450139) Szymańska A

Szymańska A

resulting in alterations in gene expression and the induction of cell differentiation

3 μM) induces 50% degradation of endogenous SGK3 within 2 hours

or on src tyrosine kinases at concentrations as high as 50 μM

Chemical Name: 1-(tert-butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3

EHop-016 at (LY450139) Szymańska AEHop 016 is a novel potent and selective inhibitor of RAC. EHop 016 inhibits Rac activity in the MDA MB 435 metastatic cancer cells that overexpress Rac and exhibits high endogenous Rac activity. The IC(50) of 1. 1 M for Rac inhibition by EHop 016 is ~ 100 fold lower than for NSC23766. EHop 016 is specific for Rac1 and Rac3 at concentrations of < 5 M. At higher concentrations, EHop 016 inhibits the close homolog Cdc42. EHop 016 also inhibits the Rac