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PHPS1 phosphatase inhibitor

Cat.No.S9913

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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 465.44 Formula

C21H15N5O6S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 314291-83-3 -- Storage of Stock Solutions

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

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (199.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Mechanism of Action

Targets/IC50/Ki
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. 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]
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]
References

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