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PTP Inhibitor I

Catalog No.
C3607
tyrosine phosphatase (PTP) inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$42.00
In stock
5g
$53.00
In stock
10g
$101.00
Ship with 10-15 days
25g
$172.00
Ship with 10-15 days
50g
$319.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

KI: 43 and 42 μM for SHP-1 and PTP1B, respectively.

PTP Inhibitor I is a tyrosine phosphatase (PTP) inhibitor.

Protein tyrosine phosphatases (PTPs) are considered to be involved in the etiology of diabetes mellitus, neural diseases such as Alzheimer’s and Parkinson’s disease, regulation of allergy and inflammation. PTPs are also considered to be responsible for the pathogens’ virulence.

In vitro: In previous study, the corresponding values of PTP Inhibitor I against PTP1B were determined to be KI of 42 μM, kinact of 0.57 min-1, and kinact/KI of 1.4*104 M-1 min-1, respectively. This study also showed that α-bromoacetophenone such as PTP Inhibitor I could provide an effective, neutral pY mimetic inhibitor of PTPs. While perturbation of the electronic properties of the phenyl ring did not significantly improve its potency against PTPs, attachment of a proper peptidyl moiety to the para position could improve both the potency and the selectivity substantially. In addition, since the covalent PTP inhibitor complex could be cleaved to regenerate the PTP activity photolytically, PTP Inhibitor I might provide a novel class of photolytic switch for controlling cellular signaling processes [1].

In vivo: Currently, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Arabaci G, Yi T, Fu H, Porter ME, Beebe KD, Pei D.  alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: structure-Activity relationship. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3047-50.

Chemical Properties

StorageStore at RT
M.Wt215.0
Cas No.2491-38-5
FormulaC8H7BrO2
Synonymsα-Bromo-4-hydroxyacetophenone|2-Bromo-4'-hydroxyacetophenone|4-Hydroxyphenacyl bromide|Protein Tyrosine Phosphatase Inhibitor I|SHP-1 Inhibitor II
Solubility≥11.5mg/mL in DMSO
Chemical Name2-bromo-1-(4-hydroxyphenyl)-ethanone
SDFDownload SDF
Canonical SMILESOC1=CC=C(C(CBr)=O)C=C1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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