Sigma-Aldrich Eya2 Phosphatase Inhibitor

Assay

≥97% (HPLC)

Quality Level

100

Form

solid

Potency

2.0 μM K_i

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 (K _D= 6.1 or 2.0 µM, respectively, with or without 5 mm exogenous mg²⁺;K _D= 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; K_D= 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: yesPrimary Target
Eya2 C-terminal Eya domain (ED) protein tyrosine phosphataseReversible: 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany