1384864-80-5
中文名称
NCGC00249987
英文名称
NCGC00249987
CAS
1384864-80-5
分子式
C16H11FN4O2S
分子量
342.35
MOL 文件
1384864-80-5.mol
更新日期
2023/03/20 15:41:25
![1384864-80-5 结构式](/CAS/20210111/GIF/1384864-80-5.gif)
基本信息
中文别名
化合物 T12194 英文别名
NCGC00249987NCGC00249987,NCGC-00249987
Benzoic acid, 3-fluoro-, 2-[[5-(2-pyrimidinylthio)-2-furanyl]methylene]hydrazide
常见问题列表
生物活性
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。靶点
IC50: 3 μM (Eya2 ED) and 6.9 μM (MBP-Eya2 FL)
体外研究
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
2+
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.