NCGC00249987 是一种高度选择性和变构 Eya2 的 Tyr 磷酸酶活性的抑制剂，对 Eya2 ED 和 MBP-Eya2 FL 的 IC₅₀ 分别为 3 μM 和 6.9 μM。NCGC00249987 专门针对肺癌细胞的迁移，侵袭伪足形成和侵袭。

NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC 50 s 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.

Solid

IC50: 3 μM (Eya2 ED) and 6.9 μM (MBP-Eya2 FL)

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. 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.

In Vitro: DMSO : < 1 mg/mL (insoluble or slightly soluble)