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531085 Eya2 Phosphatase Inhibitor, MLS000544460 - CAS 352336-36-8 - Calbiochem

A cell-permeable inhibitor of Eya2 ED tyrosine phosphatase (IC₅₀ = 4.1 µM; KD = 2.0 µM for hEya2, catalytic domain)

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Sinonimi: 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

Primary Target: Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase
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531085
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CAS #Empirical Formula
352336-36-8C₁₇H₁₂FN₃O₂S

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5310850001
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      Description
      OverviewA 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.
      Catalogue Number531085
      Brand Family Calbiochem®
      Synonyms3-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
      References
      ReferencesKrueger, A.B., et al. 2014. J. Biol. Chem. 289, 16349.
      Krueger, A.B., et al. 2013. J. Biomol. Screen. 18, 85.
      Product Information
      CAS number352336-36-8
      FormBeige solid
      Hill FormulaC₁₇H₁₂FN₃O₂S
      Chemical formulaC₁₇H₁₂FN₃O₂S
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetEya2 C-terminal Eya domain (ED) protein tyrosine phosphatase
      Primary Target K<sub>i</sub>2.0 µ
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Numero di catalogo GTIN
      5310850001 04055977242591