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PHPS1 Sodium

Catalog No. T25953 CAS 1177131-02-0

Synonyms: PHPS1 Na, PHPS1 Sodium salt

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].

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PHPS1 Sodium, CAS 1177131-02-0

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 931.00
50 mg	6-8 weeks	$ 1,210.00
100 mg	6-8 weeks	$ 1,830.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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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, at a concentration of 30 μM and over a period of 6 days, has been shown to inhibit the proliferation of various human tumor cells. Additionally, when applied at concentrations ranging from 5 to 20 μM for durations between 5 to 360 minutes, PHPS1 specifically suppresses the phosphorylation of Erk1/2 in a dose-dependent manner, without affecting Akt and Stat3 phosphorylation. In a Cell Viability Assay using human cancer cell lines including MDA-MB-435, HCT-116, HCT-15, PC-3, HT-29, NCI-H661, and Caki-1, a 30 μM concentration of PHPS1 for 6 days resulted in varying reductions in cell numbers, with no effect (0%) on Caki-1 and up to a 74% reduction in HT-29 cells. Western Blot Analysis on Madin-Darby canine kidney (MDCK) cells treated with 5, 10, and 20 μM PHPS1 for 5 to 360 minutes indicated that PHPS1 inhibited HGF/SF-induced phosphorylation of Erk1/2 within 15 minutes to 6 hours, though transient phosphorylation of Erk1/2 after 5 minutes remained unaffected. The compound showed no influence on the HGF/SF-induced activation of PI3K/Akt or Stat3.
In vivo	PHPS1 (3 mg/kg; i.p. injection; daily during the last week of the high-fat diet) significantly reduced atherosclerosis (AS) susceptibility in Ldlr -/- mice[2]. Using the Ldlr -/- (005061) mouse model[2], at a dosage of 3 mg/kg administered intraperitoneally (i.p.) daily in the final week of a high-fat diet, a marked decrease in aortic atherosclerotic plaque size was observed compared to the control groups.

Synonyms	PHPS1 Na, PHPS1 Sodium salt
Molecular Weight	488.43
Formula	C21H15N5NaO6S
CAS No.	1177131-02-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

PHPS1 Sodium 1177131-02-0 PHPS1 Na PHPS-1 Sodium PHPS1 Sodium salt inhibitor inhibit

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