PHPS1 phosphatase inhibitor

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.97

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other phosphatase Inhibitors	Osunprotafib (ABBV-CLS-484) SHP099 Hydrochloride RMC-4550 SHP099 GSK2830371 β-Glycerophosphate sodium salt hydrate Batoprotafib (TNO155) NSC87877 TPI-1 Sanguinarine chloride

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	1 year-80°Cin solvent 1 month-20°Cin solvent
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
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Shp2 (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 signalling, 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 leukaemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumour cell lines.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18480264/ [2] https://pubmed.ncbi.nlm.nih.gov/29703160/

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Chemical Structure

Molecular Weight: 465.44