531085 Eya2 Phosphatase Inhibitor, MLS000544460 - Calbiochem

531085
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₂FN₃O₂S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31085.0001
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          Glass bottle 25 mg
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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
          FormBeige solid
          Hill FormulaC₁₇H₁₂FN₃O₂S
          Chemical formulaC₁₇H₁₂FN₃O₂S
          ReversibleY
          Applications
          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
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Eya2 Phosphatase Inhibitor, MLS000544460 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Krueger, A.B., et al. 2014. J. Biol. Chem. 289, 16349.
          Krueger, A.B., et al. 2013. J. Biomol. Screen. 18, 85.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision31-July-2014 JSW
          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
          DescriptionA 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 (KD = 6.1 or 2.0 µM, respectively, with or without 5 mM exogenous Mg2+; KD = 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.
          FormBeige solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₁₂FN₃O₂S
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesKrueger, A.B., et al. 2014. J. Biol. Chem. 289, 16349.
          Krueger, A.B., et al. 2013. J. Biomol. Screen. 18, 85.