PHPS1

Catalog No.S9913 Synonyms: PTP Inhibitor V

For research use only.

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

PHPS1 Chemical Structure

CAS No. 314291-83-3

Purity & Quality Control

Choose Selective phosphatase Inhibitors

Biological Activity

Description

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

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

PHPS1 inhibits Shp2-dependent cellular events such as hepatocyte growth factor/scatter factor (HGF/SF)-induced epithelial cell scattering and branching morphogenesis. PHPS1 also blocks Shp2-dependent downstream signaling, namely HGF/SF-induced sustained phosphorylation of the Erk1/2 MAP kinases and dephosphorylation of paxillin. Furthermore, PHPS1 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]

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 PHPS1. 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 PHPS1.[2]

Protocol (from reference)

Cell Research:

[1]

  • 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 PHPS1 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 PHPS1. Total cell lysates are immunoblotted with antibodies specific for hemagglutinin epitope (HA), phospho-Erk1/2 (P-Erk1/2), and Erk1/2.

  • (Only for Reference)
Animal Research:

[2]

  • Animal Models: Ldlr−/− mice
  • Dosages: 3 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 93 mg/mL
(199.81 mM)
Ethanol 93 mg/mL
(199.81 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 465.44
Formula

C21H15N5O6S

CAS No. 314291-83-3
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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