Home Metabolism phosphatase inhibitor PHPS1

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PHPS1 phosphatase inhibitor

PHPS1 (PTP Inhibitor V), a potent and cell-permeable inhibitor, is specific for Shp2 with Ki value of 0.73 μM.

PHPS1 phosphatase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 465.44

Purity & Quality Control

Batch: S991301 DMSO]93 mg/mL]false]Ethanol]93 mg/mL]false]Water]Insoluble]false Purity: 99.97%
99.97

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Mechanism of Action

Targets
Shp2 [1]
(Cell-free assay)
0.73 μM(Ki)

In vitro
In vitro

PHPS1 inhibits Shp2-dependent cellular events such as hepatocyte growth factor/scatter factor (HGF/SF)-induced epithelial cell scattering and branching morphogenesis. This compound also blocks Shp2-dependent downstream signaling, namely HGF/SF-induced sustained phosphorylation of the Erk1/2 MAP kinases and dephosphorylation of paxillin. Furthermore, it efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.[1]
Cell Research Cell lines MDCK cells, NIH 3T3 cells, HEK293 cells
Concentrations 10 μM, 20 μM
Incubation Time 2 days
Method

MDCK cells are either untreated or treated with 20 μM PHPS1 and stimulated with 1 unit/ml of HGF/SF. Paxillin is immunoprecipitated from total cell lysates and immunoblotted with antibodies specific for paxillin and for phosphotyrosine. NIH 3T3 cells are transfected with an expression vector for RasV12 and either untreated or treated with 10 μM this compound for 2 days, respectively. Total cell lysates are immunoblotted with antibodies specific for phospho-Erk1/2 (P-Erk1/2) and Erk1/2. HEK293 cells are transfected with expression vectors for HA-GAB2, HA-SHP2-E76K, or ERBB2 and either untreated or treated with 20 μM this chemical. Total cell lysates are immunoblotted with antibodies specific for hemagglutinin epitope (HA), phospho-Erk1/2 (P-Erk1/2), and Erk1/2.

In Vivo
In vivo

PHPS1 decreases the number of atherosclerotic plaques without significantly affecting body weight, serum glucose levels or lipid metabolism. Plaque composition analysis shows a significant decrease in the number of VSMCs in atherosclerotic lesions of Ldlr−/− mice treated with this compound. Stimulation with oxLDL induces a dose-dependent increase in the number of VSMCs and in SHP2 and ERK phosphorylation levels, and these effects are blocked by this chemical.[2]
Animal Research Animal Models Ldlr−/− mice
Dosages 3 mg/kg
Administration i.p.

References
  • https://pubmed.ncbi.nlm.nih.gov/18480264/
  • https://pubmed.ncbi.nlm.nih.gov/29703160/

Chemical Information

Molecular Weight 465.44 Formula

C21H15N5O6S
CAS No. 314291-83-3 SDF --
Synonyms PTP Inhibitor V
Smiles O[S](=O)(=O)C1=CC=C(N\N=C2/C(=O)N(N=C2C3=CC=C(C=C3)[N+]([O-])=O)C4=CC=CC=C4)C=C1

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (199.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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