MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity[1].
MLS000544460 does not bind Eya3 phosphatase (ED)[1]. MLS000544460 (10 μM) inhibits Eya2-mediated cell migration in human Eya2, Eya2 phosphatase-dead (D274N), and YFP (as a negative control) expressing MCF10A cells[1]. When Eya2 ED is dialyzed into 10 μM EDTA to remove Mg2+, it binds MLS000544460 with a higher affinity (Kd=0.80 μM), indicating that this class of compounds does not require Mg2+ for its interaction with the Eya2 ED[1].
[1]. Krueger AB, et al. Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cellmigration. J Biol Chem. 2014 Jun 6;289(23):16349-61.