PTP Inhibitor V, PHPS1 is 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 µM, respectively). PHPS1 inhibits ECPTP, PTP1B, Shp1, mycobacterium MptpA only at higher concentrations (IC50 = 5.4, 19, 30, and 39 µM, respectively) and exhibits little activity against PTPH1, STEP, PTPN7, PTPRK, GLEPP1, or LAR2 even at concentrations as high as 50 µM. PTP Inhibitor V, PHPS1 has been shown to inhibit Shp-2-dependent cellular signaling and tumor cell colonies formation.
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