1384864-80-5

1384864-80-5 structure
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
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
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