A selective SHP-2 inhibitor
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PHPS1 is a cell-permeable, phosphotyrosine mimetic that inhibits the Src homology region 2 domain-containing phosphatase (SHP)-2 (IC50 = 2.1 μ Ki = 0.73 µM). 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 µM, respectively). PHPS1 has been shown to inhibit SHP-2-dependent cellular signaling and tumor cell colony formation.
Reference:
[1]. Hellmuth, K., Grosskopf, S., Lum, C.T., et al. Specific inhibitors of the protein tyrosine phosphatase Shp2 identified by high-throughput docking. Proceedings of the National Academy of Sciences of the United States of America 105(20), 7275-7280 (2008).
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