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

P 22077 

Cat. No.: HY-13865 Purity: 99.97%
Handling Instructions

P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It 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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 103 In-stock
Estimated Time of Arrival: December 31
10 mg USD 94 In-stock
Estimated Time of Arrival: December 31
50 mg USD 354 In-stock
Estimated Time of Arrival: December 31
100 mg USD 523 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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

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    • References

    • Customer Review

    Description

    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It 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].

    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].

    Molecular Weight

    315.32

    Formula

    C₁₂H₇F₂NO₃S₂

    CAS No.

    1247819-59-5

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (158.57 mM; Need ultrasonic)

    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
    10 mM 0.3171 mL 1.5857 mL 3.1714 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    P 22077P22077P-22077DeubiquitinaseDUBsInhibitorinhibitorinhibit

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    Product name:
    P 22077
    Cat. No.:
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