5.31085

MLS000544460

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

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₇H₁₂FN₃O₂S
• CAS-Nummer: 352336-36-8
• Molekulargewicht: 341.36
• MDL number: MFCD28064079
• UNSPSC Code: 12352200
• NACRES: NA.77

Eigenschaften

• Produktname: Eya2 Phosphatase Inhibitor, MLS000544460,
• 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

Beschreibung

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.

Biochem/physiol Actions

Cell permeable: yes

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

Reversible: yes

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.

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable