1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. P 22077

P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.

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

P 22077 Chemical Structure

P 22077 Chemical Structure

CAS No. : 1247819-59-5

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 113 In-stock
Solution
10 mM * 1 mL in DMSO USD 113 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 103 In-stock
50 mg USD 389 In-stock
100 mg USD 575 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    P 22077 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2017 Dec;13(12):1207-1215.  [Abstract]

    The effects of HBX19818 on FLT 3 expression in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment. The effects of P22077 on FLT 3 levels in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.

    IC50 & Target

    EC50: 8.01 μM (USP7), 8.74 μM (USP47)[1]

    In Vitro

    P 22077 is an inhibitor of USP7 and DUB USP47, with EC50s of 8.01 μM and 8.74 μM, respectively. P 22077 (15-45 μM) inhibits a much smaller subset of DUBs. P 22077 (25 μM) causes DUBs inhibition in HEK293T cells[1]. P 22077 (0-20 μM) greatly reduces the cell viability of Neuroblastoma (NB) cells including IMR-32, NGP, CHLA-255, and SH-SY5Y cells but without NB-19 and SK-N-AS cells. P 22077 (10 μM) increases p53 activity and induces apoptosis in p53 wild-type and HDM2-expressing NB cells. P 22077 (5 μM) enhances the cytotoxic effect of Dox and VP-16 on NB cells, and enhances Dox- and VP-16-induced p53-mediated apoptosis[2].

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

    In Vivo

    P 22077 (15 mg/kg, i.p. 21 days) shows potent antitumor activities in an xenograft mouse model bearing IMR-32-derived tumors; P 22077 also exhibits antitumor effects after treatment at 10 mg/kg for 14 days in mice bearing SH-SY5Y-derived tumors, and at 20 mg/kg for 12 days in mice bearing NGP-derived tumors[2].

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

    Molecular Weight

    315.32

    Formula

    C12H7F2NO3S2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=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 : 50 mg/mL (158.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1714 mL 15.8569 mL 31.7138 mL
    5 mM 0.6343 mL 3.1714 mL 6.3428 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
    =
    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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.93 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (15.86 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

    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]

    Recombinant full length USP7, USP2 core, USP5, JOSD2, DEN1, PLpro core, and SENP2 catalytic core are generated. Amino terminal His6 tagged USP4, USP8, USP28, UCH-L1, UCH-L3, UCH-L5, and MMP13 are expressed in Escherichia coli. N-terminal His6 tagged USP15, USP20, and USP47 are expressed in Sf9 cells. All the recombinant proteins are purified by chromatography. Amino terminal tagged His6 Ub-PLA2 (Ub-CHOP), SUMO3-PLA2 (SUMO3-CHOP), ISG15-PLA2 (ISG15-CHOP), NEDD8-PLA2 (NEDD8-CHOP), Ub-EKL (Ub-CHOP2), and free catalytically active PLA2 are prepared[1].

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

    Cell Assay
    [2]

    Cell viability assays are assessed using the Cell Counting Kit-8 (CCK-8, WST-8[2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2 H-tetrazolium, monosodium salt]). Cells are seeded in 96-well flat-bottomed plates at the density of 1 × 104 per well. After 24 h of incubation at 37°C, increasing concentrations of P 22077, Dox, VP-16, or their combinations are added to the wells. Twenty-four hours later, 10 μL of CCK-8 is added into each well and after 1 h of incubation, the absorbance is measure at 450 nm using the microplate reader. Each experiment is performed in replicates of six. Background reading of media only is used to normalize the results[2].

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

    Animal Administration
    [2]

    The orthotopic Neuroblastoma (NB) mouse model is used in the assay. Briefly, 1.5 × 106 human IMR-32, SH-SY5Y, or NGP cells with luciferase expression are surgically injected into the left renal capsule of 5-week-old female NCR nude mice. IMR-32, SH-SY5Y, and NGP-derived xenografts are allowed to grow for ~2-3 weeks before randomizing the mice into a control group and a P 22077 treatment group. Each group consists of three or six mice. Animals are treated with DMSO or P 22077 by intraperitoneal (i.p.) injection every day for 12, 14, or 21 days. At the end of the experiments, all mice are killed. Tumors and the right side control kidneys are resected, weighed, and photographed[2].

    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 3.1714 mL 15.8569 mL 31.7138 mL 79.2845 mL
    5 mM 0.6343 mL 3.1714 mL 6.3428 mL 15.8569 mL
    10 mM 0.3171 mL 1.5857 mL 3.1714 mL 7.9285 mL
    15 mM 0.2114 mL 1.0571 mL 2.1143 mL 5.2856 mL
    20 mM 0.1586 mL 0.7928 mL 1.5857 mL 3.9642 mL
    25 mM 0.1269 mL 0.6343 mL 1.2686 mL 3.1714 mL
    30 mM 0.1057 mL 0.5286 mL 1.0571 mL 2.6428 mL
    40 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9821 mL
    50 mM 0.0634 mL 0.3171 mL 0.6343 mL 1.5857 mL
    60 mM 0.0529 mL 0.2643 mL 0.5286 mL 1.3214 mL
    80 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9911 mL
    100 mM 0.0317 mL 0.1586 mL 0.3171 mL 0.7928 mL
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    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.

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    Cat. No.:
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