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

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.

CAS No. : 1919853-46-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of PTP1B-IN-2:

PTP1B-IN-2 Related Antibodies

Top Publications Citing Use of Products

    PTP1B-IN-2 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Mar 30;42(4):112314.  [Abstract]

    IB using pY99 to detect phosphorylated CD3ζ immunoprecipitated from Jurkat cells treated with PTP1B-IN2 (1 μM, 24 h).

    PTP1B-IN-2 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Mar 30;42(4):112314.  [Abstract]

    CAR T tumor killing assay was applied to examine the cytotoxicity of human T cells targeting Raji cells expressing GFP upon compound treatments, 1 μM PTP1B-IN2, 1 μM Palbo, or 10 μM BSJ-03–123 was applied.

    PTP1B-IN-2 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Mar 30;42(4):112314.  [Abstract]

    Bioluminescence images of tumor progression in Raji tumor-bearing mice with/without receiving CAR T cells under treatment with BSJ-03–123 (50 mg/kg) or PTP1B-IN2 (5 mg/kg).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    PTP1B-IN-2 Related Antibodies
    Molecular Weight

    680.79

    Formula

    C34H36N2O9S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (146.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4689 mL 7.3444 mL 14.6888 mL 36.7220 mL
    5 mM 0.2938 mL 1.4689 mL 2.9378 mL 7.3444 mL
    10 mM 0.1469 mL 0.7344 mL 1.4689 mL 3.6722 mL
    15 mM 0.0979 mL 0.4896 mL 0.9793 mL 2.4481 mL
    20 mM 0.0734 mL 0.3672 mL 0.7344 mL 1.8361 mL
    25 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4689 mL
    30 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
    40 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9181 mL
    50 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7344 mL
    60 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 mL
    80 mM 0.0184 mL 0.0918 mL 0.1836 mL 0.4590 mL
    100 mM 0.0147 mL 0.0734 mL 0.1469 mL 0.3672 mL
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    PTP1B-IN-2 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PTP1B-IN-21919853-46-5PhosphataseInhibitorinhibitorinhibit

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