2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Proteasome Deubiquitinase
  4. Capzimin

Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

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

Capzimin Chemical Structure

Capzimin Chemical Structure

CAS No. : 2084868-04-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 165 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Capzimin:

Capzimin Related Antibodies

Top Publications Citing Use of Products

    Capzimin purchased from MedChemExpress. Usage Cited in: Prostate. 2019 Aug;79(11):1304-1315.   [Abstract]

    22RV1 and PC3 cells are treated with or without Capzimin (5 μM) for 48 hours, and the indicated proteins are detected by Western blot analysis.

    View All Deubiquitinase Isoform Specific Products:

    View All Isoforms
    USP1 USP2 USP7 USP8 USP30 UCHL1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

    IC50 & Target

    Target: Rpn11[1]
    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    3.8 μM
    Compound: 35
    Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay
    Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay
    		[PMID: 28191850]
    HEK-293T IC50
    2.1 μM
    Compound: 35
    Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay
    Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay
    		[PMID: 28191850]
    HeLa IC50
    0.6 μM
    Compound: 35
    Inhibition of 26S proteasome regulatory subunit RPN11 deubiquitinating activity in beta5 inhibitor MG132 pretreated human HeLa cells expressing UbG76V-GFP assessed as reduction in UbG76V-GFP degradation rate by fluorescence microscopic method
    Inhibition of 26S proteasome regulatory subunit RPN11 deubiquitinating activity in beta5 inhibitor MG132 pretreated human HeLa cells expressing UbG76V-GFP assessed as reduction in UbG76V-GFP degradation rate by fluorescence microscopic method
    		[PMID: 28191850]
    In Vitro

    Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC50=30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI50 is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI50 values of 0.67 μM and 1 μM respectively), as well as several solid tumor cell lines including NCI-H460 (non-small cell lung cancer; GI50= 0.7 μM) and MCF7 (breast cancer; GI50=1.0 μM). Immunoblotting for the processed form of caspase 3 and caspase-cleaved poly ADP-ribose polymerase in HCT116 cells confirm that Capzimin not only blocks cell growth, but also induces apoptosis[1].

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

    Capzimin Related Antibodies
    Molecular Weight

    628.81

    Formula

    C30H24N6O2S4
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(C1=CC2=CC=CC(SSC3=C4N=CC(C(NCCC5=NC=CS5)=O)=CC4=CC=C3)=C2N=C1)NCCC6=NC=CS6
    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 : ≥ 55.67 mg/mL (88.53 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 1.5903 mL 7.9515 mL 15.9031 mL
    5 mM 0.3181 mL 1.5903 mL 3.1806 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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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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 (3.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.98 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.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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: 99.21%

    SDS (252 KB)

    COA (247 KB) LCMS (93 KB)

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

    Fluorescence polarization assays are performed in low-volume 384 well solid black plates in quadruplicate. The assays are performed in buffer containing 50 mM Tris-HCl pH7.5, 1mM MgCl2, 50 μM ATP, 1 mM DTT and 0.01% NP-40. The components for the assay are added in the follow sequence: 1) 5 μL compound (Capzimin, et al.) (in 3% DMSO) at different concentrations, 2) 5 μL of diluted human 26S proteasome, and 3) 5μL of substrate (3 nM Ub4- peptideOG). 100 μM Zn(cyclen)2+ is present in the titration reaction for the experiments performed with Zn(cyclen)2+. Fluorescence polarization is measured at 30°C with excitation at 480 nm and emission at 520 nm. Collected data is normalized to DMSO control and fitted to a dose-response curve to determine the IC50 value[1].

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

    HCT116 cells are treated with different concentrations of 3021 or Capzimin for 72 hours in normal or low serum medium and then mixed with CellTiter-Glo reagent to estimate cell proliferation. Measured luminescence values are normalized to DMSO control and data are fitted to a dose-response equation to determine the GI50[1].

    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 1.5903 mL 7.9515 mL 15.9031 mL 39.7576 mL
    5 mM 0.3181 mL 1.5903 mL 3.1806 mL 7.9515 mL
    10 mM 0.1590 mL 0.7952 mL 1.5903 mL 3.9758 mL
    15 mM 0.1060 mL 0.5301 mL 1.0602 mL 2.6505 mL
    20 mM 0.0795 mL 0.3976 mL 0.7952 mL 1.9879 mL
    25 mM 0.0636 mL 0.3181 mL 0.6361 mL 1.5903 mL
    30 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3253 mL
    40 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9939 mL
    50 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL
    60 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6626 mL
    80 mM 0.0199 mL 0.0994 mL 0.1988 mL 0.4970 mL
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    Capzimin 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:

    Capzimin2084868-04-0ProteasomeDeubiquitinaseDUBsInhibitorinhibitorinhibit

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