MLS000544460是一种高度选择性和可逆的Eya2磷酸酶抑制剂，Kd为2.0μM，IC50为4μM。MLS000544460抑制Eya2磷酸酶介导的细胞迁移，并具有抗癌活性。
货号:ajcx31718
CAS:352336-36-8
分子式:C17H12FN3O2S
分子量：341.36
溶解度:DMSO: 125 mg/mL (366.18 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.