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PTP Inhibitor I phosphatase inhibitor

Cat.No.S3696

PTP Inhibitor I is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor with Ki values of 43 and 42 μM for SHP-1(ΔSH2) and PTP1B, respectively.
PTP Inhibitor I phosphatase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 215.04

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

Quality Control

Batch: S369601 DMSO]43 mg/mL]false]Ethanol]43 mg/mL]false]Water]Insoluble]false Purity: 99.21%
99.21

Chemical Information, Storage & Stability

Molecular Weight 215.04 Formula

C8H7BrO2

 Storage (From the date of receipt)
CAS No. 2491-38-5 Download SDF Storage of Stock Solutions

Synonyms α-Bromo-4-hydroxyacetophenone, 2-Bromo-4'-hydroxyacetophenone, 4-Hydroxyphenacyl bromide, SHP-1 Inhibitor II Smiles C1=CC(=CC=C1C(=O)CBr)O

Solubility

In vitro
Batch:

DMSO : 43 mg/mL ( (199.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 43 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
PTP1B [1]
(Cell-free assay)
42 μM(Ki)
SHP-1(ΔSH2) [1]
(Cell-free assay)
43 μM(Ki)
In vitro
PTP Inhibitor I binds to PTPs with the highest affinity, having Ki values of 43 and 42 μM and Kinact values of 0.40 and 0.57/min for SHP-1(△SH2) and PTP1B, respectively. It has lower affinity to wild-type SHP-1 than its catalytic domain (K= 530 vs 43 μM), likely due to the fact that the SH2 domains can directly bind to the PTP active site and interfere with substrate/inhibitor binding[1].
References

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