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TCS 401 is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B; Ki = 0.29 µM).1 It inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 at much higher concentrations (Kis = 59, 560, 1,100, >2,000, >2,000, and >2,000 μM, respectively).1 Several PTPs have been proposed to act as negative regulators of insulin signaling, thus this enzyme is a potential drug target in diabetes.
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