MLS-544460
Eya2 phosphatase inhibitor / MLS-544460 is an allosteric inhibitor of the Eya2 tyrosine phosphatase (IC50=4.1 uM)1-2 which is ineffective against other tyrosine phosphatases including Eya3 and PTP1B. Treatment of patient-derived glioma stem cells induced loss of bipolar spindle formation along with G2/M cell cycle arrest. GSC proliferation was inhibited at concentrations 4 to 10-fold lower than normal brain cells.3 Treatment of Axolotls following amputation impairs limb regeneration indicating a role for Eya2 in vertebrate regeneration.4
Biochemicals & reagents
352336-36-8
MLS000544460
1 Kreuger et al. (2014), Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cell migration; J. Biol. Chem. 289 16349 2 Kreuger et al. (2013), Identification of a selective small-molecule inhibitor series targeting the eyes absent 2 (Eya2) phosphatase activity; J. Biomol. Screen. 18 85 3 Zhang et al. (2021), Targeting EYA2 tyrosine phosphatase activity in glioblastoma stem cells induces mitotic catastrophe; J. Exp. Med. 218 e20202669 4 Sousounis et al. (2020), Eya2 promotes cell cycle progression by regulating DNA damage response during vertebrate limb regeneration; Elife 289 e51217
-20°C
TARGET: Phosphatase -- PATHWAY: Cell cycle -- RESEARCH AREA: Cancer stem cells; Stem cells -- DISEASE AREA: Cancer