|Description||EHop-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 μM 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 μM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells. EHop-016 holds promise as a targeted therapeutic agent for the treatment of metastatic cancers with high Rac activity.|
|Synonyms||EHop-016; EHop016; EHop 016; EHOP-016; EHOP016; EHOP 016|
EHop-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 e...
EHT 1864 is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively.
ML141 is a potent, selective and reversible non-competitive inhibitor of Rho family GTPase cdc42 with IC50 of 200 nM.
NSC 23766 is a specific inhibitor of the binding and activation of RAC GTPase. It does not inhibit the closely related targets, Cdc42 or RhoA.
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