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A selective SHP-2 inhibitor
PHPS1 is a cell-permeable, phosphotyrosine mimetic that inhibits the Src homology region 2 domain-containing phosphatase (SHP)-2 (IC50 = 2.1 ?M; Ki = 0.73 ?M).1 It is selective for SHP-2, inhibiting ECPTP, PTP1B, SHP-1, and mycobacterium MptpA at relatively higher concentrations (IC50s = 5.4, 19, 30, and 39 ?M, respectively).1 PHPS1 has been shown to inhibit SHP-2-dependent cellular signaling and tumor cell colony formation.1
1.Hellmuth, K., Grosskopf, S., Lum, C.T., et al.Specific inhibitors of the protein tyrosine phosphatase Shp2 identified by high-throughput dockingProc. Natl. Acad. Sci. USA105(20)7275-7280(2008)
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