NCGC00249987 |
| カタログ番号GC61403 |
NCGC00249987 は、Eya2 ED および MBP-Eya2 FL の IC50 が 3 μM および 6.9 μM である、Eya2 阻害剤の高度に選択的かつアロステリックな Tyr ホスファターゼ活性です。 NCGC00249987 は、肺癌細胞の移動、浸潤突起形成、および浸潤を特に標的としています。
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Cas No.: 1384864-80-5
Sample solution is provided at 25 µL, 10mM.
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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].
[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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