1. Metabolic Enzyme/Protease
    Autophagy
  2. Proteasome
    Autophagy

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

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

Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
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50 mg USD 108 In-stock
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100 mg USD 180 In-stock
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200 mg USD 288 In-stock
Estimated Time of Arrival: December 31
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Customer Review

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

    H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Bortezomib purchased from MCE. Usage Cited in: Patent. US20160222465A1.

    Impact of Ibrutinib on p-AKT, ERK and BTK expression following SDF-1a stimulation of plenti-GFP vector, CXCR4WT and CXCR4S338X expressing BCWM.1 cells. plenti-GFP vector, CXCR4WT and CXCR4S338X expressing BCWM.1 cells are pretreated for 2 hours with either Ibrutinib (0.5 uM) or AMD3100 (30 uM) prior to stimulation with SDF-1a (20 nM) for 2 minutes. Results depict differences in phospho-AKT, phospho-ERK, and phospho-BTK obtained by immunoblotting follow

    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: Patent. US20160222465A1.

    CXCR4S338X expressing BCWM.1 and MWCL-1 cells show variable resistance to PARP and caspase 3 cleavage mediated by WM relevant therapeutics in the presence of SDF-1a, and reversed by AMD3100. plenti-GFP vector, CXCR4WT and CXCR4S338X expressing WM cells are treated for 6 hours with Bendamustine (BENDA), Fludarabine (FLUDARA), Bortezomib (BORT), and Idelalisib (IDELA) at their EC50 doses in the presence or absence of SDF-1a (20 nM) and/or the CXCR4 recep

    Bortezomib purchased from MCE. Usage Cited in: Nat Commun. 2017 May 22;8:15398.

    HEK293T cells are treated with 50 μg/mL Cycloheximide and increasing concentrations of Lenalidomide, Thalidomide or with DMSO, and cells are incubated for 6 h. ZFP91 and GAPDH levels are detected using anti-ZFP91 or anti-GAPDH immunoblotting.

    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.

    Western blot analysis of ER stress-related proteins after PPI treatment for 48 h in both pH 7.4 and pH 6.5 conditions. Cells treated with Thapsigargin (TG, 0.5 and 1 μM) or Tunicamycin (Tu, 2.5, 5 and 10 μg/mL) for 24 h served as positive controls.

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

    AGS cells transfected with HA-tagged SQSTM1 plasmid, are treated with 25 μg/mL Cycloheximide (CHX) over a 240-min time period or treated with 100 μg/mL PPI for 48 h in pH 7.4 conditions, and then followed by 25 μg/mL CHX over a 240-min time period.

    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: Mol Plant Pathol. 2018 Jul 26.

    Destabilization of BRC1 mediated by SWP1 is inhibited by proteasome inhibitors Epoxomicin and MG132.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

    IC50 & Target

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

    In Vitro

    Bortezomib (PS-341) effects proteins that control cell cycle progression. Treatment of PC-3 cells with Bortezomib (100 nM) for 8 h results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. The Bortezomib doses at which 50% of PC-3 cells are killed at 24 and 48 h are determined to be 100 and 20 nM, respectively[1]. Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome. Inhibition of the proteasome by Bortezomib results in activation of JNK, stabilization of p53, Bid, Bax, p21, p27, caveolin-1, and IκBα, resulting in inhibition of NF-κB[2]. The IC50 of Bortezomib is found to be 2.46 nM for 26S proteasome in the B16F10 cells[3].

    In Vivo

    Mice bearing PC-3 tumors are treated with Bortezomib (i.v., 0.3 or 1.0 mg/kg). Bortezomib (1.0 mg/kg) results in a significant decrease in tumor growth ~60%. Bortezomib (0.3 mg/kg) produces a 16% decrease in tumor volume but did not reach significance[1]. Bortezomib (0.2 mg/kg) significantly decreases the withdrawal threshold on days 11 and 15 and increases the number of withdrawal responses on days 11 and 15 compared with the vehicle group in the von Frey and acetone tests[4].

    Clinical Trial
    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.
    References
    Cell Assay
    [1]

    The human PC-3 prostate tumor cells are treated with Bortezomib (0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM) for 24-48 h in complete medium. Cytotoxicity is measured using a MTT assay[1].

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

    Animal Administration
    [1][4]

    Mice[1]
    Male nude mice (18-20 g; n=51) are used. Bortezomib (0.3 or 1.0 mg/kg) is administered in vehicle i.v. using a dose volume of 100 μL per mouse or directly into the tumor in a 10 μL volume. Due to the comparatively high levels of Bortezomib in the prostate, after i.v. dosing of radiolabeled drug, it is decided to examine the effects of this novel compound in the prostate, PC-3, xenograft tumor model. Animals are treated when the tumors become palpable (>300 mm3). Male nude mice (18-20 g; n=51) are used. Bortezomib (0.3 or 1.0 mg/kg) is administered in vehicle i.v. using a dose volume of 100 μL per mouse or directly into the tumor in a 10 μL volume. Due to the comparatively high levels of Bortezomib in the prostate, after i.v. dosing of radiolabeled drug, it is decided to examine the effects of this novel compound in the prostate, PC-3, xenograft tumor model. Animals are treated when the tumors become palpable (>300 mm3).
    Rats[4]
    Male Sprague-Dawley rats weighing 200-250 g are used. Bortezomib (0.05, 0.1, or 0.2 mg/kg) or vehicle (5% DMSO solution) is administered intraperitoneally (i.p.) twice a week for 2 weeks (on days 1, 4, 8, and 11). The administration schedule and doses of Bortezomib are determined based on clinical treatment (1.3 mg/m2 of Bortezomib on days 1, 4, 8, and 11).

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

    References
    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

    Storage

    4°C, protect from light

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.97%

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    Product Name:
    Bortezomib
    Cat. No.:
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    Bortezomib

    Cat. No.: HY-10227