Eya2 Phosphatase Inhibitor, MLS000544460-Calbiochem

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一般描述

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 ?M; 100 nM ED & 5 ?M Mg²⁺; Substrate = 25 ?M OMFP) via affinity docking at an allosteric pocket located opposite to the active site (K_D= 6.1 or 2.0 ?M, respectively, with or without 5 mM exogenous Mg²⁺;K_D= 0.8 ?M 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 ?M 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 ?M.
A cell-permeable furylidenebenzohydrazide compound that acts as an inhibitor of Eya2 ED tyrosine phosphatase (IC₅₀= 4.1 ?M; K_D= 2.0 ?M for hEya2, catalytic domain at 5 ?M 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 ?M). 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 ?M) it has a mixed type inhibition. Reduces Eya2-mediated cell migration in MCF10A cells (~ 10 ?M).

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

生化/生理作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

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

法律信息

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

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