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Beschreibung

A cell-permeable phosphotyrosine mimetic that acts as a reversible, active-site targeting, substrate-competitive inhibitor of Shp-2 (IC50 and Ki = 2.1 and 0.73 µ,M, respectively). PHPS1 inhibits ECPTP, PTP1B, Shp1, mycobacterium MptpA only at higher concentrations (IC50 = 5.4, 19, 30, and 39 µ,M, respectively) and exhibits little activity against PTPH1, STEP, PTPN7, PTPRK, GLEPP1, or LAR2 even at concentrations as high as 50 µ,M. Shown to inhibit Shp-2-dependent cellular signaling and tumor cell colonies formation.