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.
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Bortezomib Chemical Structure
CAS No. : 179324-69-7
This product is a controlled substance and not for sale in your territory.
Based on 150 publication(s) in Google Scholar
Other Forms of Bortezomib:
Bortezomib-d8
In-stock
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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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.
Bortezomib Related Antibodies
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.
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
ConcentrationSolventMass
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
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.
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.
Protocol 3
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
This protocol yields a clear solution of ≥ 4 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 EtOH stock solution (40.0 mg/mL) to 900 μLCorn oil, and mix evenly.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 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 7
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 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 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22.
[Content Brief]
[2]. Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24.
[Content Brief]
[3]. Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64.
[Content Brief]
[4]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9.
[Content Brief]
[5]. Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80.
[Content Brief]
[6]. Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18.
[Content Brief]
[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22.
[2]. Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24.
[3]. Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64.
[4]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9.
[5]. Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80.
[6]. Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18.
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
ConcentrationSolventMass
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
Bortezomib Related Classifications
Metabolic Enzyme/ProteaseNF-κBApoptosisAutophagy
ProteasomeNF-κBApoptosisAutophagy
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