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 (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.
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)
| assay | ≥97% (HPLC) |
| Quality Level | 100 |
| form | solid |
| potency | 2.0 μM Ki |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | beige |
| solubility | DMSO: 100 mg/mL |
| storage temp. | 2-8°C |
