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

Bortezomib (Synonyms: PS-341; Brotezamide; DPBA; LDP 341; MG 341; Radiciol; NSC 681239)

Cat. No.: HY-10227 Purity: 99.97%
Handling Instructions

Bortezomib (PS-341) is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib (PS-341) disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib (PS-341) is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans.

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Bortezomib Chemical Structure

Bortezomib Chemical Structure

CAS No. : 179324-69-7

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Customer Review

Based on 26 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Bortezomib purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7. pii: e38430.

    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 MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.

    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 MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.

    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 MCE. Usage Cited in: Eur J Pharmacol. 2017 Nov 15;815:147-155.

    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).

    Bortezomib purchased from MCE. Usage Cited in: BMC Cancer. 2018 Oct 11;18(1):971.

    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 MCE. Usage Cited in: Clin Cancer Res. 2019 Jun 15;25(12):3630-3642.

    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.
    • Biological Activity

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    Description

    Bortezomib (PS-341) is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib (PS-341) disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib (PS-341) is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans[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].

    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].

    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.

    179324-69-7

    SMILES

    OB(O)[[email protected]](CC(C)C)NC([[email protected]@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: 

    DMSO : ≥ 83.3 mg/mL (216.79 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2603 mL 1.3013 mL 2.6025 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

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

    Purity: 99.97%

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