| Description | PHPS1 sodium is a potent and selective inhibitor of Shp2, 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]. |
| In vitro | PHPS1 (30 μM; 6 days) inhibits human tumor cells proliferation[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) Concentration: 30 μM Incubation Time: 6 days Result: Resulted in a reduction in cell number of between 0% (Caki-1) to 74% (HT-29). Western Blot Analysis [1] Cell Line: Madin-Darby canine kidney (MDCK) cells Concentration: 5, 10, 20 μM Incubation Time: 5, 15, 60, 120, 360 minutes Result: Inhibited HGF/SF (1 unit/mL)-induced phosphorylation and thus activation of Erk1/2 over a time period of 15 min to 6 h. In contrast, transient phosphorylation of Erk1/2 after 5 min was not affected. Exhibited no effect on HGF/SF-induced activation of PI3K/Akt or Stat3. |
| In vivo | PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) made Ldlr -/- mice less prone to atherosclerosis(AS)[2]. Animal Model: Ldlr -/- (005061) mice [2] Dosage: 3 mg/kg Administration: Intraperitoneal (i.p.) injection; every day during the last week on the high-fat diet. Result: Revealed a significant decrease in atherosclerotic plaque size in the aorta compared with the other two groups. |
| Synonyms | PHPS1 Na, PHPS1 Sodium salt |
| molecular weight | 488.43 |
| Molecular formula | C21H15N5NaO6S |
| CAS | 1177131-02-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Chen J, Cao Z, Guan J. SHP2 inhibitor PHPS1 protects against atherosclerosis by inhibiting smooth muscle cell proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72. doi: 10.1186/s12872-018-0816-2. PubMed PMID: 29703160; PubMed Central PMCID: PMC5923012. 2. Salem IH, Plante S, Gounni AS, Rouabhia M, Chakir J. A shift in the IL-6/STAT3 signalling pathway imbalance towards the SHP2 pathway in severe asthma results in reduced proliferation process. Cell Signal. 2018 Mar;43:47-54. doi: 10.1016/j.cellsig.2017.12.001. Epub 2017 Dec 11. PubMed PMID: 29242170. 3. Zhou W, Yin Y, Weinheimer AS, Kaur N, Carpino N, French JB. Structural and Functional Characterization of the Histidine Phosphatase Domains of Human Sts-1 and Sts-2. Biochemistry. 2017 Sep 5;56(35):4637-4645. doi: 10.1021/acs.biochem.7b00638. Epub 2017 Aug 21. PubMed PMID: 28759203; PubMed Central PMCID: PMC5907918. 4. Qiu Z, Zhou J, Liu F, Qin X, Dai Y, Ke Y, Chen Z, Li W, Ying S, Shen H. Deletion of Shp2 in bronchial epithelial cells impairs IL-25 production in vitro, but has minor influence on asthmatic inflammation in vivo. PLoS One. 2017 May 8;12(5):e0177334. doi: 10.1371/journal.pone.0177334. eCollection 2017. PubMed PMID: 28481957; PubMed Central PMCID: PMC5421800. |