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PTP1B-IN-2 (Synonyms: Protein Tyrosine Phosphatase 1B Inhibitor 2)

Catalog No.GC31324

PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.

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PTP1B-IN-2 Chemical Structure

Cas No.: 1919853-46-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$203.00
In stock
1mg
$45.00
In stock
5mg
$135.00
In stock
10mg
$189.00
In stock
50mg
$567.00
In stock
100mg
$882.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

PTP1B-IN-2 is predispensed in 96-well microplates as 1.0 µL aliquots per well in 100% DMSO. The PTP1B enzymatic assay is carried out in a total volume of 100 µL per well in assay plates with 15 nM recombinant PTP1B protein, 2 mM p-nitrophenylphosphonic acid (pNPP), 1 mM dithiothreitol and 1 mM EDTA (pH 6.5). After 30 min incubation at 37oC, the reaction is terminated by addition of 2.5 M NaOH. The amount of hydrolysis product, pNP, is monitored by detection of the absorbance at 405 nm[1].

References:

[1]. Liu P, et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity. Eur J Med Chem. 2016 Aug 8;118:27-33.

Background

PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.

PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several hydrogen bonds and hydrophobic interactions with key residues of the catalytic site. The binding characteristics between PTP1B domain and ligand shows that PTP1B-IN-2 is an ABC type inhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 µM and 30 µM. Insulin-stimulated glucose uptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%, 19.0% and 38.1% at 5, 10 and 20 µM, respectively [1].

[1]. Liu P, et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity. Eur J Med Chem. 2016 Aug 8;118:27-33.

Chemical Properties

Cas No. 1919853-46-5 SDF
Synonyms Protein Tyrosine Phosphatase 1B Inhibitor 2
Canonical SMILES O=S(N(C1=CC(C(OC)=O)=C(OCC2=CC=C(C)C=C2)C=C1)CC3=CC=C(N(S(C)(=O)=O)CC(OC)=O)C=C3)(CC4=CC=CC=C4)=O
Formula C34H36N2O9S2 M.Wt 680.79
Solubility DMSO : ≥ 100 mg/mL (146.89 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.4689 mL 7.3444 mL 14.6888 mL
5 mM 0.2938 mL 1.4689 mL 2.9378 mL
10 mM 0.1469 mL 0.7344 mL 1.4689 mL
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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.
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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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