2. Protein Tyrosine Kinase/RTK
  3. Src
  4. PP2

PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.

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

PP2 Chemical Structure

PP2 Chemical Structure

CAS No. : 172889-27-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 87 In-stock
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10 mg USD 145 In-stock
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Customer Review

Based on 43 publication(s) in Google Scholar

PP2 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE PP2

WB
IF

    PP2 purchased from MedChemExpress. Usage Cited in: FASEB J. 2020 Aug;34(8):10443-10461.  [Abstract]

    Cells are pretreated with PP2 (10 μM) for 24 hours and further treated with MMS, and GAPDH nuclear translocation is visualized by confocal microscopy. The immunofluorescence staining results directly show that inhibiting Src activity by PP2 decreases GAPDH nuclear distribution in response to MMS.

    PP2 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 May;109(5):1648-1659.  [Abstract]

    Cells are treated with vehicle (0.1% DMSO) or PP2 (2.5 μM and 5 μM) for 48 h. Cell lysates are harvested. Total and phosphorylated c-Src are detected by western blotting.

    PP2 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 May 12;22(8):3768-3781.  [Abstract]

    Prostate cancer cells are grown and treated with different concentrations of the Src inhibitor PP2 for 2 h and subjected to Western blot analysis. The data show that the inhibition of Src dose dependently decreases levels of p-Src527 but not p-Src426.

    PP2 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.  [Abstract]

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.

    PP2 purchased from MedChemExpress. Usage Cited in: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Jul;27(7):568-73.  [Abstract]

    To determine whether the inhibition of caveolin-1 tyrosine residues 14 ( Cav-1-Y14 ) phosphorylation with protein tyrosine kinase inhibitors ( PP2 ) will upregulate heme oxygenase-1 ( HO-1 ) activity to protect against ventilation induced lung injury in vivo of an animal model. The group D1 or D2 receive high tidal volume ventilation for 1 hour or 2 hour respectively, but they are given PP2 1 hour before high tidal volume ventilation. The groups E1 and E2 also receive high tidal volume ventilat

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.

    IC50 & Target

    IC50: 4 nM (Lck), 5 nM (Fyn)[1]
    In Vitro

    At 10 μM, the effect of PP2 on cellular proliferation is not significant, indicating that, at this low concentration, the effect of PP2 on Gemcitabine cytotoxicity does not simply reflect a direct antiproliferative effect, but rather a potentiation of Gemcitabine-induced cytotoxicity. Above 20 μM, growth is increasingly suppressed, a finding consistent with reports in other human cancer cell lines. Although 10 μM PP2 is used in our study, at higher concentrations PP2 is reported to inhibit other intracellular kinases[2]. PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50 of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture[3].

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

    PP2 Related Antibodies
    In Vivo

    The tumor growth inhibition rate is 25% in the PP2 treatment group and 5% in the Gemcitabine treatment group (P>0.05). When administered in combination, PP2 and Gemcitabine produce a tumor growth inhibition rate of 98% (P<0.05). Hepatic metastasis occurred in 100% of control and Gemcitabine-treated groups; 88% of the PP2-treated group developed liver metastases. There are no detectable metastases in the group treated with PP2 and Gemcitabine in combination (P<0.05)[2].

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

    301.77

    Formula

    C15H16ClN5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(Cl)C=C3)=NC=N1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (165.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3138 mL 16.5689 mL 33.1378 mL
    5 mM 0.6628 mL 3.3138 mL 6.6276 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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

    ×
    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    90% Corn Oil

      Solubility: ≥ 3 mg/mL (9.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 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 (30.0 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
    Cell Assay
    [2]

    Cell growth is determined by MTT assay and confirmed by cell counting. Results of the MTT assay have been shown to correlate well with [3H]thymidine incorporation in pancreatic cancer cell lines. Logarithmically growing cells are plated at 5×103 cells/well in 96-well plates, allowed to adhere for 24 h, and cultured in the presence or absence of PP2 and Gemcitabine. Cell proliferation is determined after 96 h. Plates are read using a Vmax microplate spectrophotometer at a wavelength of 570 nm corrected to 650 nm and normalized to controls. Each independent experiment is performed three times, with 10 determinations for each condition tested. The IC50 of Gemcitabine is calculated from these results. At identical time points, cells are trypsinized to form a single cell suspension. Intact cells, determined by trypan blue exclusion, are counted using a Neubauer hemocytometer, and the number of cells per mL is calculated and compared with the control group to confirm the MTT results[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Male athymic nu/nu mice (age, 5 weeks; weight, 20-22 g; specific pathogen free) are anesthetized with i.p. ketamine (200 mg/kg) and xylazine (10 mg/kg) and inoculated with 106 Gemcitabine-resistant PANC1GemRes cells in 20 μL of PBS by surgical orthotopic implantation into the pancreas. After inoculation, mice are randomized to three treatment groups: (a) treatment group 1 (n=8) receive 2 mg/kg PP2 in 1% DMSO by i.p. injection three times a week; (b) treatment group 2 (n=8) receive Gemcitabine (100 mg/kg) in the same volume of 1% DMSO vehicle as received by group 1, three times a week; and (c) treatment group 3 (n=8) receive 2 mg/kg PP2 and 100 mg/kg Gemcitabine in the same volume of DMSO as groups 1 and 2, three times a week. The control group receive the same volume of 1% DMSO vehicle as the other groups, three times a week. Treatment is commenced 1 day after implantation, and necropsy is performed 4 weeks after implantation. Primary tumors are identified, weighed, and normalized to total body mass. Tumor growth inhibition rate is calculated using the following formula: tumor growth inhibition rate (%)=(1−MT/MC)×100, where MT and MC are the mean normalized tumor masses of treatment and control groups, respectively. Liver metastases are counted and confirmed histologically.

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3138 mL 16.5689 mL 33.1378 mL 82.8446 mL
    5 mM 0.6628 mL 3.3138 mL 6.6276 mL 16.5689 mL
    10 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2845 mL
    15 mM 0.2209 mL 1.1046 mL 2.2092 mL 5.5230 mL
    20 mM 0.1657 mL 0.8284 mL 1.6569 mL 4.1422 mL
    25 mM 0.1326 mL 0.6628 mL 1.3255 mL 3.3138 mL
    30 mM 0.1105 mL 0.5523 mL 1.1046 mL 2.7615 mL
    40 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.0711 mL
    50 mM 0.0663 mL 0.3314 mL 0.6628 mL 1.6569 mL
    60 mM 0.0552 mL 0.2761 mL 0.5523 mL 1.3807 mL
    80 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0356 mL
    100 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8284 mL
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    PP2 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:

    PP2172889-27-9AGL 1879PP 2PP-2AGL1879AGL-1879SrcInhibitorinhibitorinhibit

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