1. Metabolic Enzyme/Protease NF-κB Apoptosis Autophagy
  2. Proteasome NF-κB Apoptosis Autophagy
  3. Bortezomib

Bortezomib  (Synonyms: PS-341; LDP-341; NSC 681239)

Cat. No.: HY-10227 Purity: 99.83%
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Bortézomib (PS-341) est un protéasome inhibiteur réversible et sélectif, et inhibe puissamment le protéasome 20S (Ki=0,6 nM) en ciblant sur un résidu de thréonine. Bortézomib perturbe le cycle cellulaire, induit l'apoptose et inhibe NF-κB. Bortézomib est le premier inhibiteur thérapeutique du protéasome utilisé chez l'homme. L'activité anticancéreuse.

Bortezomib (PS-341) ist ein reversibler und selektiver proteasome-Inhibitor und hemmt das 20S proteasome (Ki=0.6 nM) stark, indem es auf einen Threonin-Rest abzielt. Bortezomib stört den Zellzyklus, induziert Apoptose und hemmt NF-κB. Anti-Krebs-Aktivität.

Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.

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

Bortezomib Chemical Structure

Bortezomib Chemical Structure

CAS No. : 179324-69-7

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Customer Review

Based on 126 publication(s) in Google Scholar

Other Forms of Bortezomib:

Top Publications Citing Use of Products

118 Publications Citing Use of MCE Bortezomib

IF
WB
Proliferation Assay

    Bortezomib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2023 May 19.  [Abstract]

    Bortezomib (BTZ; 5, 10, 20 nM; 48 h) increases the expression level of γH2AX in RPMI-8226 and U266 cells.

    Bortezomib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2023 May 19.  [Abstract]

    Bortezomib (BTZ; 10 nM; 48 h) significantly enhances the cell death of RPMI-8226.

    Bortezomib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2019 Jun 15;25(12):3630-3642.  [Abstract]

    H1975 cells treated with 5 μmol/L MTI-31 alone or in combination with 10 μmol/L CQ or 0.01 μmol/L PS-341.

    Bortezomib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.  [Abstract]

    AGS cells are pretreated with 25 and 50 nM Bortezomib for 1 h, and then incubated with 500 nM Torin 1 for 24 h. After pretreatment with PPI for 24 h in pH 7.4 or pH 6.5 condition, Rapamycin (1 μM) or Torin 1 (500 nM) is added for another 24 h. The protein level of SQSTM1 is measured by western blot analysis.

    Bortezomib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.  [Abstract]

    Different concentrations of two classical proteasome inhibitors Bortezomib and MG132 are added. AGS cells are either untreated or treated with Bortezomib (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).

    Bortezomib purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Bortezomib purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2018 Oct 11;18(1):971.  [Abstract]

    The reduction of MAGEC2 protein level in TRIM28-knockdown A375 cells can be inhibited by treatment with both MG132 and PS-341, and similar result is also observed in Hs 695 T cells.

    Bortezomib purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2017 Nov 15;815:147-155.  [Abstract]

    Shown are GFPu fluorescent images of the GFPu-HEK293 cells treated with CuSO4 (Cu, 20 μM), HK (20 μM), HK-Cu (HC, 20 μM), or Velcade (Vel, 100 nM).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

    IC50 & Target

    Ki: 0.6 nM (20S proteasome)[1]

    In Vitro

    Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1[1].
    ? Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines[3].
    ? Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines[3].
    ? The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells[4].
    ? Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3)[5].

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

    Cell Cycle Analysis[1]

    Cell Line: PC-3 cells
    Concentration: 100 nM
    Incubation Time: 8 hours
    Result: Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.

    Apoptosis Analysis[3]

    Cell Line: JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)
    Concentration: 5-100 nM
    Incubation Time: 20 hours
    Result: The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).

    Western Blot Analysis[3]

    Cell Line: wtp53 (Granta-519), mutp53 (Jeko) cells
    Concentration: 20 nM
    Incubation Time: 1, 2, 4, 6, 14 hours
    Result: Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).
    In Vivo

    Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice[1].

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

    Animal Model: Male nude mice (xenograft tumor model bearing PC-3 cells)[1]
    Dosage: 0.3, 1 mg/kg
    Administration: Intravenous injection; once weekly for 4 weeks
    Result: Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.
    Clinical Trial
    Molecular Weight

    384.24

    Formula

    C19H25BN4O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    Ethanol : 66.67 mg/mL (173.51 mM; ultrasonic and warming and heat to 60°C)

    DMSO : 50 mg/mL (130.13 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 2.6025 mL 13.0127 mL 26.0254 mL
    5 mM 0.5205 mL 2.6025 mL 5.2051 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (40.0 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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: 99.97%

    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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 2.6025 mL 13.0127 mL 26.0254 mL 65.0635 mL
    5 mM 0.5205 mL 2.6025 mL 5.2051 mL 13.0127 mL
    10 mM 0.2603 mL 1.3013 mL 2.6025 mL 6.5064 mL
    15 mM 0.1735 mL 0.8675 mL 1.7350 mL 4.3376 mL
    20 mM 0.1301 mL 0.6506 mL 1.3013 mL 3.2532 mL
    25 mM 0.1041 mL 0.5205 mL 1.0410 mL 2.6025 mL
    30 mM 0.0868 mL 0.4338 mL 0.8675 mL 2.1688 mL
    40 mM 0.0651 mL 0.3253 mL 0.6506 mL 1.6266 mL
    50 mM 0.0521 mL 0.2603 mL 0.5205 mL 1.3013 mL
    60 mM 0.0434 mL 0.2169 mL 0.4338 mL 1.0844 mL
    80 mM 0.0325 mL 0.1627 mL 0.3253 mL 0.8133 mL
    100 mM 0.0260 mL 0.1301 mL 0.2603 mL 0.6506 mL
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    • 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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