1384864-80-5

1384864-80-5 structure

Name: NCGC00249987
Chemical Name: NCGC00249987
CAS Number: 1384864-80-5
Molecular Formula: C₁₆H₁₁FN₄O₂S
Molecular Weight: 342.35
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
Create Date: 2020-06-02 04:37:37
Modify Date: 2024-01-09 18:17:39
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].

Name	NCGC00249987

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase
Target	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].
References	[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.

Molecular Formula	C₁₆H₁₁FN₄O₂S
Molecular Weight	342.35