NCGC00249987

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NCGC00249987  纯度: 99.86%

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。

NCGC00249987

NCGC00249987 Chemical Structure

CAS No. : 1384864-80-5

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NCGC00249987 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

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 & Target

IC50: 3 μM (Eya2 ED) and 6.9 μM (MBP-Eya2 FL)[1]
体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

342.35

Formula

C16H11FN4O2S
CAS 号

1384864-80-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)
参考文献

  • [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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