2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. Deubiquitinase Autophagy Apoptosis
  4. PR-619

PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.

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

CAS No. : 2645-32-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 38 publication(s) in Google Scholar

PR-619 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE PR-619

WB
Histological Imaging/Staining
IP

    PR-619 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Sep 30;20(13):5254-5271.  [Abstract]

    C3H/10T1/2 cells pre-treated with AM were intervened with CHX in the presence of or PR-619 (15 μM, 48 h).

    PR-619 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Sep 30;20(13):5254-5271.  [Abstract]

    C3H/10T1/2 cells were co-incubated with or without AM in the presence of PR-619 for 48 hours, followed by IP with anti-β-catenin and IB with indicated antibodies.

    PR-619 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 May 20;81(1):221.  [Abstract]

    The hematoxylin-stained ovary sections of control and PR-619 (75 µM, 48 h) mice. The boxed region of each figure was magnified accordingly. Scale bar: 100 μm.

    PR-619 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jan;30(1):168-183.  [Abstract]

    Immunoblot analysis of NLRP3 and GAPDH in LPS-primed (Mock) FAAH-/- BMDMs, with or without co-treatment of PYR41 (5 μM) or PR619 (5 μM).

    PR-619 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jan;30(1):168-183.  [Abstract]

    Immunoblotting analysis showing the protein levels of Kif5B in control, PR-619-treated.PR-619 (10 μM) was used to treat GV oocytes for 22 hours, respectively.

    View All Deubiquitinase Isoform Specific Products:

    View All Isoforms
    USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis[1][2][3][4].

    IC50 & Target

    EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)[1]
    In Vitro

    PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation[2].
    PR-619 affects the microtubule network and led to the accumulation of small punctuated tau deposits around. PR-619 causes the dephosphorylation of tau[3].
    PR-619 (7-12.5 μM) causes an increase in the abundance of ubiquitinated proteins within 24 h. PR-619 leads to the induction of heat shock proteins and to an increase of ubiquitinated proteins[3].
    PR-619 (9 μM) affects the organization of the microtubule network in OLN-t40 cells[3].
    PR-619 (5, 7.5, and 10 μM) induces ER Stress and ER-Stress related apoptosis on T24 and BFTC-905 cells. PR-619 induces polyubiquitination, Bcl-2 downregulation, and concurrent PARP cleavage in a dose-dependent manner. PR-619 induces G0/G1 arrest in UC cells[4].

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

    PR-619 Related Antibodies

    Cell Cytotoxicity Assay[1]

    Cell Line: OLN-t40 cells.
    Concentration: 0-10 μM.
    Incubation Time: 24 hours.
    Result: Exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM.
    In Vivo

    PR-619 (10 mg/kg/day) enhances the antitumor effect of Cisplatin on a Cisplatin-Na ve and Cisplatin-resistant UC Xenograft of nude mice[4].

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

    Animal Model: Nude mice[4].
    Dosage: 10 mg/kg/day (Cisplatin combined).
    Administration: Intraperitoneally.
    Result: Enhanced the antitumor effect of Cisplatin.
    Molecular Weight

    223.28

    Formula

    C7H5N5S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    NC1=C(SC#N)C=C(SC#N)C(N)=N1
    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 : ≥ 21 mg/mL (94.05 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 4.4787 mL 22.3934 mL 44.7868 mL
    5 mM 0.8957 mL 4.4787 mL 8.9574 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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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    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 (11.20 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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.
    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

    Purity: 99.38%

    SDS (396 KB)

    COA (250 KB) LCMS (102 KB)

    Handling Instructions (2659 KB)
    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 4.4787 mL 22.3934 mL 44.7868 mL 111.9670 mL
    5 mM 0.8957 mL 4.4787 mL 8.9574 mL 22.3934 mL
    10 mM 0.4479 mL 2.2393 mL 4.4787 mL 11.1967 mL
    15 mM 0.2986 mL 1.4929 mL 2.9858 mL 7.4645 mL
    20 mM 0.2239 mL 1.1197 mL 2.2393 mL 5.5984 mL
    25 mM 0.1791 mL 0.8957 mL 1.7915 mL 4.4787 mL
    30 mM 0.1493 mL 0.7464 mL 1.4929 mL 3.7322 mL
    40 mM 0.1120 mL 0.5598 mL 1.1197 mL 2.7992 mL
    50 mM 0.0896 mL 0.4479 mL 0.8957 mL 2.2393 mL
    60 mM 0.0746 mL 0.3732 mL 0.7464 mL 1.8661 mL
    80 mM 0.0560 mL 0.2799 mL 0.5598 mL 1.3996 mL
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    PR-619 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:

    PR-6192645-32-1PR619PR 619DeubiquitinaseAutophagyApoptosisDUBsG0/G1arrestER-stresstauubiquitinationInhibitorinhibitorinhibit

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