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Chemical Structure : NCGC00249987
Catalog No.: 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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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.
| M.Wt | 342.348 | |
| Formula | C16H11FN4O2S | |
| Appearance | Solid | |
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1. Jothi Anantharajan, et al. Mol Cancer Ther. 2019 Sep;18(9):1484-1496.
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