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MLS000544460

Chemical Structure : MLS000544460

CAS No.: 352336-36-8

MLS000544460 (EYA2i)

Catalog No.: PC-72461Not For Human Use, Lab Use Only.

MLS000544460 (EYA2i) is a specific, allosteric inhibitor of Eya2 phosphatase with IC50 of 4.1 uM, KD of 2.0 uM, does not bind Eya3 ED, Eya1 and Eya4 ED.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MLS000544460 (EYA2i) is a specific, allosteric inhibitor of Eya2 phosphatase with IC50 of 4.1 uM, KD of 2.0 uM, does not bind Eya3 ED, Eya1 and Eya4 ED.
MLS000544460 inhibits Eya2-mediated cell migration.
MLS000544460 decreased mesenchymal phenotypes and enhanced cancer cell immunogenicity, resulting in attenuated tumor growth and metastasis.
MLS000544460 treatment increased infiltration of cytotoxic T and NK cells, and enhanced anti-PD-1 therapy response in mouse tumor models.
Inhibition of the EYA2 Tyr phosphatase activity via MLS000544460, mimicked EYA2 loss in glioblastoma stem cells (GSCs) in vitro and extended the survival of tumor-bearing mice.

Physicochemical Properties

M.Wt 341.36
Formula C17H12FN3O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-Fluorobenzoic acid 2-[[5-(2-pyridinylthio)-2-furanyl]methylene]hydrazide

References

1. Zhang G, et al. J Exp Med. 2021 Nov 1;218(11):e20202669.

2. Jia Z Shen, et al. Mol Cell. 2022 Feb 11;S1097-2765(22)00087-9.

3. Krueger AB, et al. J Biol Chem. 2014 Jun 6;289(23):16349-61.

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