PTP Inhibitor I is a cell-permeable protein tyrosine phosphatase (PTP) inhibitor, it binds to PTPs with Ki values of 43 and 42 μM and Kinact values of 0.40 and 0.57/min for SHP-1(△SH2) and PTP1B, respectively.
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PTP Inhibitor I is a photoreversible covalent Inhibitor of PTP (Protein Tyrosine Phosphatases) with Ki value of 42μM for PTP1B. PTP Inhibitor I 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 I 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. Treatment with PTP Inhibitor I>300μM resulted in the hyperphosphorylation of a protein at 110 kDa in human B cells post 3min, consistent with inhibition of a PTP(s) which normally dephosphorylates this protein. Also it decreased the phosphorylation level of a 50 kDa protein at concentrations as low as 30μM.
作用机制
PTP Inhibitor I could bind to the PTP active site as a phosphotyrosine mimetic.[1]
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