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Eya2ED和MBP-Eya2FL的IC50分别为3μM和6.9μM。NCGC00249987专门针对肺癌细胞的迁移，侵袭伪足形成和侵袭。
货号:ajcx31708
CAS:1384864-80-5
分子式:C16H11FN4O2S
分子量：342.35
溶解度:DMSO:< 1 mg/mL (insoluble or slightly soluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.