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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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Synonyme: 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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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
352336-36-8C₁₇H₁₂FN₃O₂S

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      		 Glasflasche 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
      CAS number352336-36-8
      FormBeige solid
      Hill FormulaC₁₇H₁₂FN₃O₂S
      Chemical formulaC₁₇H₁₂FN₃O₂S
      ReversibleY
      Quality LevelMQ100
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5310850001 04055977242591

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Krueger, A.B., et al. 2014. J. Biol. Chem. 289, 16349.
      Krueger, A.B., et al. 2013. J. Biomol. Screen. 18, 85.
      Datenblatt

      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
      CAS number352336-36-8
      Chemical formulaC₁₇H₁₂FN₃O₂S
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.