NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC₅₀s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells.

NCGC00249987 inhibits Eya2 ED (C-terminal Eya Domain). NCGC00249987 inhibits full length Eya2 including but not other Eya family members.
NCGC00249987 binding leads to a conformational change of the active site that is unfavorable for Mg²⁺ binding, thereby inhibiting Eya2’s Tyr phosphatase activity.
NCGC00249987 (5, 10 μM) treatment effectively suppresses migration, invadopodia formation and invasion in Eya2 WT expressing Calu-6 cells, but not in EV Calu-6 cells. NCGC00249987 does not inhibit cell growth or survival.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Anantharajan J, et al. Structural and Functional Analyses of an Allosteric EYA2 Phosphatase Inhibitor That Has On-Target Effects in Human Lung Cancer Cells. Mol Cancer Ther. 2019 Sep;18(9):1484-1496.  [Content Brief]