NCGC00249987NCGC00249987
MedChemExpress (MCE)
HY-133512
1384864-80-5
99.91%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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.
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].
IC50: 3 μM (Eya2 ED) and 6.9 μM (MBP-Eya2 FL)[1] 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NCGC00249987 Related Antibodies
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[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. [Content Brief]