PHPS1

Catalog No.S9913 Batch:S991301

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Technical Data

Formula

C21H15N5O6S
Molecular Weight 465.44 CAS No. 314291-83-3
Solubility (25°C)* In vitro DMSO 93 mg/mL (199.81 mM)
Ethanol 93 mg/mL (199.81 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:

[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.
Animal Study:

[2]
  • Animal Models

    Ldlr−/− mice

  • Dosages

    3 mg/kg

  • Administration

    i.p.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.