EHop-016 at (LY450139) Coleman RL

Coleman RL

Szymańska A

Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin

(43):5438-40

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

EHop-016 at (LY450139) Coleman RLEHop 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