Millipore Sigma Vibrant Logo
Attention: We have moved. EMD Millipore products are no longer available for purchase on emdmillipore.com.Learn More

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)

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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
View Products on Sigmaaldrich.com
531085
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
352336-36-8C₁₇H₁₂FN₃O₂S

Products

Catalog NumberPackaging Qty/Pack
5.31085.0001 Glass bottle 25 mg
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
Catalog Number GTIN
5.31085.0001 04055977242591

Documentation

Eya2 Phosphatase Inhibitor, MLS000544460 - CAS 352336-36-8 - 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
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.