5.31085

Eya2 Phosphatase Inhibitor, MLS000544460

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₁₇H₁₂FN₃O₂S
• Número CAS: 352336-36-8
• Peso molecular: 341.36
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥97% (HPLC)
• Nível de qualidade: 100
• forma: solid
• potência: 2.0 μM K_i
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: beige
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable