PTP Inhibitor V, PHPS1 Chemical Properties

Density 

1.54±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble10mg/mL, clear (warmed)

pka

-2.90±0.40(Predicted)

form 

solid

color 

red

InChI

InChI=1S/C21H15N5O6S/c27-21-20(23-22-15-8-12-18(13-9-15)33(30,31)32)19(14-6-10-17(11-7-14)26(28)29)24-25(21)16-4-2-1-3-5-16/h1-13,22H,(H,30,31,32)

InChIKey

VIQSBJOMLQLAKC-UHFFFAOYSA-N

SMILES

C1(S(O)(=O)=O)=CC=C(NN=C2C(=O)N(C3=CC=CC=C3)N=C2C2=CC=C([N+]([O-])=O)C=C2)C=C1

Safety Information

WGK Germany 

2

PTP Inhibitor V, PHPS1 Usage And Synthesis

Description

PTP Inhibitor V, PHPS1 is a cell-permeable phosphotyrosine mimetic that acts as a reversible, active-site targeting, substrate-competitive inhibitor of SH-PTP2 (Shp-2) (IC50 and Ki = 2.1 and 0.73μM, respectively). PHPS1 inhibits PCPTP1 (ECPTP), PTP1B, SH-PTP1 (Shp1), mycobacterium MptpA only at higher concentrations (IC50 ;= 5.4, 19, 30, and 39 μM, respectively) and exhibits little activity against PTPH1, STEP, PTPN7, PTPRK, GLEPP1, or LAR2 even at concentrations as high as 50 μM. PTP Inhibitor V, PHPS1 has been shown to inhibit Shp-2-dependent cellular signaling and tumor cell colonies formation

Uses

Phenylhydrazono pyrazolone sulfonate 1 (PHPS1) sodium salt hydrate has been used as a protein-tyrosine phosphatase (shp2) inhibitor to study its effects on bisphenol A (BPA) and nonyl phenol (NP)-induced cell proliferation of MCF7 cell. It has also been used as a shp2 inhibitor to study its pro-atherosclerotic or atheroprotective effect in vivo and in vitro.

Biochem/physiol Actions

Phenylhydrazono pyrazolone sulfonate 1 (PHPS1) represses E2-induced gene transcription and rapid DNA synthesis. It also blocks mitogen-activated protein kinase (ERK1/2) activation and reduces the cigarette smoke induced-inflammatory response in mouse lungs.