2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. P005091

P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.

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

P005091 Chemical Structure

P005091 Chemical Structure

CAS No. : 882257-11-6

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Customer Review

Based on 23 publication(s) in Google Scholar

P005091 Related Antibodies

Top Publications Citing Use of Products

    P005091 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Nov 15;38(1):468.   [Abstract]

    DU145 and VCaP cells are treated with the USP7 inhibitor P5091 for 24 h, and the protein levels of USP7 and PLK1 are assessed by immunoblotting.

    P005091 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Nov 15;38(1):468.   [Abstract]

    DU145 and VCaP cells are treated with the USP7 inhibitor P5091 for 24 h, and the protein levels of USP7 and PLK1 are assessed by immunoblotting.

    P005091 purchased from MedChemExpress. Usage Cited in: Mol Carcinog. 2019 Jan;58(1):42-54.  [Abstract]

    Treatment with P5091 increases the cleavage of CASP9, CASP3, and PARP. ESCC cells Kyse450, Kyse510 and Kyse30 are treated with P5091 for 72 h and cell lysates are assessed by western blotting with specific antibodies against cleaved CASP9, CASP3, or PARP. GAPDH is used as a control.

    View All Deubiquitinase Isoform Specific Products:

    View All Isoforms
    USP1 USP2 USP7 USP8 USP10 USP30 UCHL1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.

    IC50 & Target

    EC50: 4.2 μM (USP7)
    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    11 μM
    Compound: 1, P-005091
    Cytotoxicity against human HCT116 cells after 72 hrs
    Cytotoxicity against human HCT116 cells after 72 hrs
    		[PMID: 24900381]
    Sf9 IC50
    4.2 μM
    Compound: 1, P-005091
    Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay
    Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay
    		[PMID: 24900381]
    In Vitro

    P005091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P005091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P005091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P005091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P005091. Moreover, P005091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P005091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P005091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P005091 inhibits growth in MM cells and overcomes bortezomib-resistance. P005091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6-14 μM). P005091 overcomes bone marrow stromal cell-induced growth of MM Cells. P005091 decreases HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, P005091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P005091 treatment, the cytotoxic activity of P005091 is not dependent on p53[1].

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

    P005091 Related Antibodies
    In Vivo

    In animal tumor model studies, P005091 is well tolerated, inhibits tumor growth, and prolongs survival. Combining P005091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggers synergistic anti-MM activity[1].

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

    348.22

    Formula

    C12H7Cl2NO3S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(C1=CC([N+]([O-])=O)=C(SC2=CC=CC(Cl)=C2Cl)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 : 25 mg/mL (71.79 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 2.8717 mL 14.3587 mL 28.7175 mL
    5 mM 0.5743 mL 2.8717 mL 5.7435 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.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    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.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.92%

    SDS (479 KB)

    COA (254 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Recombinant enzymes in 20 mM Tris-HCl (pH 8.0), 2 mM CaCl2, and 2 mM β-mercaptoethanol are incubated with dose ranges of P005091 for 30 min in a 96-well plate before the addition of Ub-PLA2 and NBD C6-HPC or Ub-EKL and EKL substrate. The liberation of a fluorescent product within the linear range of the assay is monitored using a Perkin Elmer Envision fluorescence plate reader. Vehicle (2% [v/v] DMSO) and 10 mM N-ethylmaleimide (NEM) are included as controls.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    For the animal study, P005091 is dissolved in 4% NMP(N-methyl-2-Pyrrolidone), 4% Tween-80, and 92% Milli-Q water at a final concentration of 2 mg/mL. The human plasmacytoma xenograft model is performed as previously described. CB-17 SCID-mice are subcutaneously inoculated with MM.1S, ARP-1, or RPMI-8226 cells in 100 μL of serum free RPMI-1640 medium. When tumors are measurable (100-180 mm3), mice are randomized into treatment groups. In the SCID-hu model, human fetal bone grafts are subcutaneously implanted into SCID mice. Four weeks after bone implantation, INA-6 cells are injected directly into the fetal bone implant in SCID mice; and as a measure of tumor burden, mouse sera samples are analyzed for shIL-6R by ELISA. Upon detection of shIL-6R, mice are treated with vehicle or P005091, and mouse serum is analyzed for alterations in shIL-6R levels.

    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 2.8717 mL 14.3587 mL 28.7175 mL 71.7937 mL
    5 mM 0.5743 mL 2.8717 mL 5.7435 mL 14.3587 mL
    10 mM 0.2872 mL 1.4359 mL 2.8717 mL 7.1794 mL
    15 mM 0.1914 mL 0.9572 mL 1.9145 mL 4.7862 mL
    20 mM 0.1436 mL 0.7179 mL 1.4359 mL 3.5897 mL
    25 mM 0.1149 mL 0.5743 mL 1.1487 mL 2.8717 mL
    30 mM 0.0957 mL 0.4786 mL 0.9572 mL 2.3931 mL
    40 mM 0.0718 mL 0.3590 mL 0.7179 mL 1.7948 mL
    50 mM 0.0574 mL 0.2872 mL 0.5743 mL 1.4359 mL
    60 mM 0.0479 mL 0.2393 mL 0.4786 mL 1.1966 mL
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    P005091 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:

    P005091882257-11-6P5091P 005091P-005091P 5091P-5091DeubiquitinaseDUBsInhibitorinhibitorinhibit

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