NCGC00249987 

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^[1].

IC50: 3 μM (Eya2 ED) and 6.9 μM (MBP-Eya2 FL)^[1]

NCGC00249987 inhibits Eya2 ED (C-terminal Eya Domain). NCGC00249987 inhibits full length Eya2 including but not other Eya family members^[1].
NCGC00249987 binding leads to a conformational change of the active site that is unfavorable for Mg²⁺ binding, thereby inhibiting Eya2’s Tyr phosphatase activity^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

342.35

C₁₆H₁₁FN₄O₂S

1384864-80-5

Solid

Off-white to light yellow

FC1=CC=CC(C(N/N=C/C(O2)=CC=C2SC3=NC=CC=N3)=O)=C1

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]