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Key Documents

5.31085

Sigma-Aldrich

Eya2 Phosphatase Inhibitor, MLS000544460

Sinónimos:

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

Fórmula empírica (notación de Hill):
C17H12FN3O2S
Número de CAS:
Peso molecular:
341.36
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥97% (HPLC)

Quality Level

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

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.
A cell-permeable furylidenebenzohydrazide compound that acts as an inhibitor of Eya2 ED tyrosine phosphatase (IC50 = 4.1 µM; KD = 2.0 µM for hEya2, catalytic domain at 5 µM Mg2+). Inhibition appears to be reversible and allosteric in nature. Does not affect the activity of Eya3, PTP1B, PPM1A, and Scp1 even at higher concentration (IC50 >100 µM). Although its binding to Eya2 ED is not Mg2+ dependent, its inhibitory activity is dependent on the concentration of Mg2+ in the medium. At higher Mg2+ levels (~5 mM) the inhibition is non-competitive whereas at low Mg2+ levels (~5 µM) it has a mixed type inhibition. Reduces Eya2-mediated cell migration in MCF10A cells (~ 10 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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