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PTP Inhibitor II

Catalog No.
C3591
protein tyrosine phosphatase (PTP) inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$42.00
In stock
25g
$61.00
Ship with 10-15 days
50g
$108.00
Ship with 10-15 days
100g
$190.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

KI: 128 μM

PTP Inhibitor II is a protein tyrosine phosphatase (PTP) inhibitor.

Protein tyrosine phosphatases (PTPs) are reported to be involved in the etiology of diabetes mellitus, neural diseases such as Alzheimer and Parkinson diseases, regulation of allergy and inflammation, or PTPs are even regarded to be responsible for the pathogens.

In vitro: In a previous study, it was found that all of the previously reported PTP inhibitors contained a negatively charged, nonhydrolyzable pY mimetic as the core structure, such as malonates, aryl carboxylates, phosphonates, or cinnamates. The poor membrane permeability of these inhibitors might compromise their potential development. It was reported that several α-bromoacetophenone derivatives, such as PTP Inhibitor II, could act as fairly potent PTP inhibitors, by covalently alkylating the conserved catalytic cysteine in the PTP active Site. Since PTP Inhibitor II is neutral, it could readily diffuse into human B cells and inhibit the intracellular PTPs. The SAR study was performed with the catalytic domain of phosphatase SHP-1, and ti was found that PTP Inhibitor II showed time-dependent inactivation of SHP-1, consistent with the mechanism. Furthermore, the potency of PTP Inhibitor II was described by an equilibrium constant KI, representing the dissociation constant of the noncovalent enzyme–inhibitor complex. PTP inhibitor II bound with lower affinity than PTP Inhibitor I with Ki values of 128 μM [1].

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

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

Reference:
[1] P.  Heneberg. Use of protein tyrosine phosphatase inhibitors as promising targeted therapeutic drugs. Current Medicinal Chemistry 16(6), 706-733 (2009).

Chemical Properties

StorageStore at RT
M.Wt229.1
Cas No.2632-13-5
FormulaC9H9BrO2
Synonymsα-Bromo-4’-methoxyacetophenone|ω-Bromo-4’-methoxyacetophenone|4-(Bromoacetyl)anisole|4-Methoxyphenacyl bromide|NSC 129010|Protein Tyrosine Phosphatase Inhibitor II
Solubilityinsoluble in H2O; ≥10.85 mg/mL in DMSO; ≥27.77 mg/mL in EtOH
Chemical Name2-bromo-1-(4-methoxyphenyl)-ethanone
SDFDownload SDF
Canonical SMILESCOC1=CC=C(C(CBr)=O)C=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control