NCGC00249987

• CAT Number: I015507
• CAS Number: 1384864-80-5
• Molecular Formula: C16H11FN4O2S
• Molecular Weight: 342.35
• Purity: ≥95%
• Synonyms: 3-fluoro-N-[(E)-(5-pyrimidin-2-ylsulfanylfuran-2-yl)methylideneamino]benzamide
• InChI: InChI=1S/C16H11FN4O2S/c17-12-4-1-3-11(9-12)15(22)21-20-10-13-5-6-14(23-13)24-16-18-7-2-8-19-16/h1-10H,(H,21,22)/b20-10+
• InChIKey: DRXIKWHRYGIZNG-KEBDBYFISA-N
• SMILES: C1=CC(=CC(=C1)F)C(=O)NN=CC2=CC=C(O2)SC3=NC=CC=N3

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].
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].

Reference

[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.
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