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Merck
CN

5.31085

MLS000544460

≥97% (HPLC), Eya2 Phosphatase Inhibitor, solid

Synonym(s):

Eya2 Phosphatase Inhibitor, MLS000544460, 3-Fluoro-N-(( E)-(5-pyridin-2-ylsulfanylfuran-2-yl)methylideneamino)benzamide, ( E)-3-Fluoro-Nʹ-((5-(pyridin-2-ylthio)furan-2-yl)methylene)benzohydrazide, Eab1 Inhibitor, Eyes Absent Homolog 2 Inhibitor

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About This Item

Empirical Formula (Hill Notation):
C17H12FN3O2S
CAS Number:
352336-36-8
Molecular Weight:
341.36
MDL number:
MFCD28064079
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

Eya2 Phosphatase Inhibitor, MLS000544460,

assay

≥97% (HPLC)

form

solid

potency

2.0 μM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

beige

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Reversible: yes
Cell permeable: yes
Primary Target
Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable furylidenebenzohydrazide compound that acts as a reversible inhibitor against Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase (PTP) activity (IC50 = 4.1 µM; 100 nM ED & 5 µM Mg2+; Substrate = 25 µM OMFP) via affinity docking at an allosteric pocket located opposite to the active site (KD = 6.1 or 2.0 µM, respectively, with or without 5 mM exogenous Mg2+; KD = 0.8 µM with 10 mM EDTA and no exogenous Mg2+), while being ineffective against the PTP activity of Eya3 & PTP1B or the Ser/Thr phosphatase activity of PPM1A & Scp1. Shown to reduce Eya2 overexpression-induced migration enhancement in MCF10A cultures (17% vs. 54% enhancement with or without 10 µM inhibitor). The inhibition appears to be non-competitive with respect to substrate in the presence of 5 mM Mg2+, while mixed mode of inhibition is observed at a low Mg2+ concentration of 5 µM.

Other Notes

Krueger, A.B., et al. 2014. J. Biol. Chem.289, 16349.

Krueger, A.B., et al. 2013. J. Biomol. Screen.18, 85.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Konstantinos Sousounis et al.
eLife, 9 (2020-03-07)
How salamanders accomplish progenitor cell proliferation while faithfully maintaining genomic integrity and regenerative potential remains elusive. Here we found an innate DNA damage response mechanism that is evident during blastema proliferation (early- to late-bud) and studied its role during tissue

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