PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].
PHPS1 (30 μM; 6 days) inhibits proliferation of human tumor cells[1]. PHPS1 (5-20 μM; 5-360 minutes) inhibits Erk1/2 but not Akt and Stat3 phosphorylation in a dose-dependent manner[1]. Cell Viability Assay[1] Cell Line: Human cancer cell lines MDA-MB-435, HCT-116 (colon carcinoma), HCT-15 (colon carcinoma), PC-3 (prostate carcinoma), HT-29 (colon carcinoma), NCI-H661 (lung carcinoma), and Caki-1 (kidney carcinoma)
PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) renders Ldlr-/- mice less susceptible to atherosclerosis development[2]. Animal Model: Ldlr-/- (005061) mice[2]
[1]. Klaus Hellmuth, et al. Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-Throughput Docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80. [2]. Jia Chen, et al. SHP2 Inhibitor PHPS1 Protects Against Atherosclerosis by Inhibiting Smooth Muscle Cell Proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72.