1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. PTP1B-IN-2

PTP1B-IN-2 

Cat. No.: HY-100462 Purity: 99.85%
Handling Instructions

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

For research use only. We do not sell to patients.

PTP1B-IN-2 Chemical Structure

PTP1B-IN-2 Chemical Structure

CAS No. : 1919853-46-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 593 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

IC50: 50 nM (PTP1B)[1]

In Vitro

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].

Molecular Weight

680.79

Formula

C₃₄H₃₆N₂O₉S₂

CAS No.

1919853-46-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (146.89 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

PTP1B-IN-2PhosphataseInhibitorinhibitorinhibit

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Product Name:
PTP1B-IN-2
Cat. No.:
HY-100462
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