Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
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- Formule: C19H25BN4O4
- Masse moléculaire:384.24
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Bortezomib (GMP) (PS-341 (GMP)) (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 (GMP) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines[3].
Bortezomib (GMP) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines[3].
The IC50 of Bortezomib (GMP) is found to be 2.46 nM for 26S proteasome in the B16F10 cells[4].
Bortezomib (GMP) 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.
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Cell Line:PC-3 cells
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Concentration:100 nM
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Incubation Time:8 hours
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Result:Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.
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Cell Line:JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)
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Concentration:5-100 nM
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Incubation Time:20 hours
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Result:The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).
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Cell Line:wtp53 (Granta-519), mutp53 (Jeko) cells
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Concentration:20 nM
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Incubation Time:1, 2, 4, 6, 14 hours
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Result:Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nude mice (xenograft tumor model bearing PC-3 cells)[1]
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Dosage:0.3, 1 mg/kg
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Administration:Intravenous injection; once weekly for 4 weeks
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Result:Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.
Chemical Information
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Masse moléculaire 384.24
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Formule C19H25BN4O4
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SMILES
OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O
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Synonyms
PS-341 (GMP); LDP-341 (GMP); NSC 681239 (GMP)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
[7]. Wang Y, et al. TREM2-Mediated Cholesterol Efflux in Macrophages Inhibits Anti-Tumor Immunity via Limitation of CD4+ T and NK Cells. Adv Sci (Weinh). 2025 Oct 20:e06995. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bortezomib (GMP) Related Classifications
HY-10227G Related Classifications
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