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NCGC00249987

Chemical Structure : NCGC00249987

CAS No.: 1384864-80-5

NCGC00249987 (Compound 9987)

货号: PC-72452Not For Human Use, Lab Use Only.

NCGC00249987 (Compound 9987) is a small-molecule allosteric inhibitor that specifically inhibits the Tyr phosphatase activity of EYA2 with IC50 of 3.1 uM (Eya2 ED), but not other Eya family members.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NCGC00249987 (Compound 9987) is a small-molecule allosteric inhibitor that specifically inhibits the Tyr phosphatase activity of EYA2 with IC50 of 3.1 uM (Eya2 ED), but not other Eya family members.
NCGC00249987 binding leads to a conformational change of the active site that is unfavorable for Mg2+ binding, thereby inhibiting Eya2's Tyr phosphatase activity. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells, it does not inhibit cell growth or survival.
NCGC00249987 has no effect on lung cancer cells carrying an Eya2 F290Y mutant.
NCGC00249987 is a useful chemical probe to study the function of the Eya2 Tyr phosphatase activity in cells, as well as an anti-metastatic agent for cancers reliant on Eya2's Tyr phosphatase activity.

物理化学性质&存储条件

分子量 342.348
分子式 C16H11FN4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-3-fluoro-N'-((5-(pyrimidin-2-ylthio)furan-2-yl)methylene)benzohydrazide

参考文献

1. Jothi Anantharajan, et al. Mol Cancer Ther. 2019 Sep;18(9):1484-1496.

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