PTP Inhibitor II is a cell-permeable protein tyrosine phosphatase (PTP) inhibitor, it covalently binds the catalytic domain of theSrc homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with Ki value of 128 μM.
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PTP Inhibitor II is a photoreversible covalent Inhibitor of PTP (Protein Tyrosine Phosphatases) with Ki value of 128μM for SHP-1(ΔSH2). PTP Inhibitor II could bind to the PTP active site as a phosphotyrosine mimetic. Its phenyl ring could engage in hydrophobic interactions with the protein as the phenyl ring of a substrate does, and the electron-rich halogen atom could mimic the negatively charged phosphate oxyanions. Binding of PTP Inhibitor II to the PTP active site in such a manner would place the R-carbon, which is highly susceptible to nucleophilic attack, next to the catalytic cysteine. An SN2 reaction between 1 and the cysteine thiol would result in the formation of a covalent enzyme-inhibitor adduct through a stable thioether linkage and loss of phosphatase activity.
作用机制
PTP Inhibitor II could bind to the PTP active site as a phosphotyrosine mimetic.[1]
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