Bortezomib (PS-341) [179324-69-7]
Cat# A2614-10mg
Size : 10mg
Brand : APExBIO Technology
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Bortezomib (PS-341)
Catalog No.
A2614
proteasome inhibitor
Featured Products
Bortezomib (PS-341; CAS 179324-69-7) is a reversible proteasome inhibitor structurally composed as an N-terminally protected dipeptide (Pyz-Phe-boroLeu) containing pyrazinoic acid, phenylalanine, and leucine with boronic acid substitution. It exerts biological activity primarily by inhibiting proteasomal degradation pathways, thereby accumulating pro-apoptotic factors and initiating programmed cell death. Bortezomib inhibits proliferation in cell-based assays, such as human non-small cell lung cancer H460 cells (IC50 = 0.1 µM). It has clinical approval for relapsed multiple myeloma and mantle cell lymphoma, and is widely employed in research to study proteasome-regulated cellular processes and apoptosis signaling pathways.
References:
1. Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.
2. Gelman JS, Sironi J, Berezniuk I, Dasgupta S, Castro LM, Gozzo FC, Ferro ES, Fricker LD (2013). "Alterations of the intracellular peptidome in response to the proteasome inhibitor bortezomib". In Gartel, Andrei L. PLoS One 8 (8): e53263.
- 1. Yingzhi Ye, Zhe Zhang, et al. "DCPS modulates TDP-43-linked neurodegeneration through P-body-mediated RNA decay." Neuron. March 09, 2026
- 2. Juncong Luo, Nini Li, et al. "Mitogen-activated protein kinase 10 suppresses non-small cell lung cancer metastasis through phosphorylation-dependent ubiquitination of keratin 16." Int J Biol Macromol. 2025 Dec 22;338(Pt 2):149740. PMID: 41435962
- 3. Laxman Nawale, Shinyeong Ju, et al. "ATE1 promotes breast cancer progression via arginylation-dependent regulation of MAPK-MYC signaling." Cell Commun Signal. 2025 Sep 2;23:390. PMID: 40898325
- 4. Nicholas W Harper, Gavin A Birdsall, et al. "RNA Pol II inhibition activates cell death independently from the loss of transcription." Cell. 2025 Aug 14:S0092-8674(25)00856-6. PMID: 40818455
- 5. Shirel Steinberger, Julia Adler, et al. "Proteasome caspase-like activity regulates stress granules and proteasome condensates." Front Cell Dev Biol. 2025 Jun 5:13:1570499. PMID: 40538982
- 6. Jiseong Kim, Yuping Zhao, et al. "Extracellular Vesicle‐Mediated Delivery of 20S Proteasomes Enhances Tau Degradation in Recipient Cells." J Extracell Vesicles. 2025 May;14(5):e70086. PMID: 40384174
- 7. Jeffrey J. Kelu, Simon M. Hughes, et al. "Muscle peripheral circadian clock drives nocturnal protein degradation via raised Ror/Rev-erb balance and prevents premature sarcopenia." Proc Natl Acad Sci U S A. 2025 May 13;122(19):e2422446122. PMID: 40324095
- 8. Anat Raiff, Shidong Zhao, et al. "TOM20 - driven E3 ligase recruitment regulates mitochondrial dynamics through PLD6." Nat Chem Biol. 2025 Apr 22. PMID: 40263465
- 9. Gayathri Samarasekera, Nancy E Go, et al. "Caspase 3 and caspase 7 promote cytoprotective autophagy and the DNA damage response during non-lethal stress conditions in human breast cancer cells." PLoS Biol.2025 Feb 21;23(2):e3003034. PMID: 39982959
- 10. Wang Jiahui, Yu Xiang, et al. "The mitochondrial DNAJC co-chaperone TCAIM reduces α-ketoglutarate dehydrogenase protein levels to regulate metabolism." Molecular Cell Volume 85, Issue 3P638-651.E9, February 06, 2025. PMID: 39889707
- 11. Brittany Q Pham, Sang Ah Yi, et al. "mTORC1 regulates the pyrimidine salvage pathway by controlling UCK2 turnover via the CTLH-WDR26 E3 ligase." Cell Rep. 2025 Jan 28;44(1):115179. PMID: 39808525
- 12. Nicholas W. Harper, Gavin A. Birdsall et al. "Pol II degradation activates cell death independently from the loss of transcription." bioRxiv. 2025 Jan 14:2024.12.09.627542. PMID: 39713309
- 13. Sitao Zhang, Sonia Vazquez-Sanchez, et al. "Acetylation of lysine 82 initiates TDP-43 nuclear loss of function by disrupting its nuclear import." bioRxiv. 07, 2024
- 14. Manuela Pérez-Berlanga, Vera I Wiersma, et al. "Loss of TDP‐43 oligomerization or RNA binding elicits distinct aggregation patterns." EMBO J. 2023 Jul 11;e111719. PMID: 37431963
- 15. Stephanie Pei Tung Yiu, Cassie Zerbe, et al. "An Epstein-Barr virus protein interaction map reveals NLRP3 inflammasome evasion via MAVS UFMylation." Mol Cell. 2023 Jul 6;83(13):2367-2386.e15. PMID: 37311461
- 16. Nuria Vilaboa, Juan Antonio Lopez, et al. "Disruption of Proteostasis by Natural Products and Synthetic Compounds That Induce Pervasive Unfolding of Proteins: Therapeutic Implications." Pharmaceuticals (Basel). 2023 Apr 19;16(4):616. PMID: 37111374
- 17. Kevin Gilhaus, Claudia Cepok, et al. "Activation of Hippo Pathway Damages Slit Diaphragm by Deprivation of Ajuba Proteins." J Am Soc Nephrol. 2023 Jun 1;34(6):1039-1055. PMID: 36930055
- 18. Ceylan B, Taşkın HB, et al. "The ERAD system is restricted by elevated ceramides." Int J Sports Physiol Perform 2023 Feb 01;18(2) PMID: 36638812
- 19. Rachel Sharninghausen, Jiwon Hwang, et al. "Identification of ERAD-dependent degrons for the endoplasmic reticulum lumen." bioRxiv. June 22, 2023
- 20. Mikhail S. Chesnokov, Marianna Halasi, et al. "Novel FOXM1 inhibitor identified via gene network analysis induces autophagic FOXM1 degradation to overcome chemoresistance of human cancer cells." Cell Death Dis. 2021 Jul 14;12(7):704 PMID: 34262016
- 21. Qi Zhu, Xu-xu Zhuang, et al. "Lycorine, a natural alkaloid, promotes the degradation of alpha-synuclein via PKA-mediated UPS activation in transgenic Parkinson's disease models." Phytomedicine. 2021 Jul;87:153578 PMID: 34038839
- 22. David Romero-Suarez, Tune Wulff, et al. "A Reporter System for Cytosolic Protein Aggregates in Yeast." ACS Synth Biol. 2021 Mar 19;10(3):466-477 PMID: 33577304
- 23. Yue Peng, Xiaofeng Sun, et al. "Role of DNA methylation on human CTSG in dermatomyositic myoideum." Cell Biol Int. 2020 Dec;44(12):2409-2415 PMID: 32813288
- 24. Dana Mamriev, Ruqaia Abbas, et al. "A small-molecule ARTS mimetic promotes apoptosis through degradation of both XIAP and Bcl-2." Cell Death Dis. 2020 Jun 25;11(6):483 PMID: 32587235
- 25. Tsai YJ, Hao CY, et al. "Expression of long pentraxin 3 in human nasal mucosa fibroblasts, tissues, and secretions of chronic rhinosinusitis without nasal polyps." J Mol Med (Berl). 2020;98(5):673-689 PMID: 32239253
- 26. Lin J, Boon L, et al. "Desensitization using imlifidase and EndoS enables chimerism induction in allosensitized recipient mice." Am J Transplant. 2020;10.1111/ajt.15851 PMID: 32185855
- 27. Haiyang Yu, Shan Lu, et al. "TDP-43 and HSP70 phase separate into anisotropic, intranuclear liquid spherical annuli." bioRxiv. March 29, 2020
- 28. Tracy Cai X, Li H, et al. "AWD regulates timed activation of BMP signaling in intestinal stem cells to maintain tissue homeostasis." Nat Commun. 2019 Jul 5;10(1):2988 PMID: 31278345
- 29. Timms RT, Zhang Z, et al. "A glycine-specific N-degron pathway mediates the quality control of protein N-myristoylation." Science. 2019 Jul 5;365(6448). pii: eaaw4912 PMID: 31273098
- 30. Rodriguez-Fernandez IA, Qi Y, et al. "Loss of a proteostatic checkpoint in intestinal stem cells contributes to age-related epithelial dysfunction." Nat Commun. 2019 Mar 5;10(1):1050 PMID: 30837466
- 31. Yuan NN, Cai CZ, et al. "Canthin-6-One Accelerates Alpha-Synuclein Degradation by Enhancing UPS Activity: Drug Target Identification by CRISPR-Cas9 Whole Genome-Wide Screening Technology." Front Pharmacol. 2019 Jan 28;10:16 PMID: 30745870
- 32. Cui-ZanCai, He-FengZhou, et al. "Natural alkaloid harmine promotes degradation of Alpha-synuclein via PKA-mediated ubiquitin-proteasome system activation." Phytomedicine. Available online 30 January 2019, 152842
- 33. SemraUnalad, SemaArslanc, et al. "Design and characterization of polycaprolactone-gelatin-graphene oxide scaffolds for drug influence on glioblastoma cells." European Polymer Journal. Volume 115, June 2019, Pages 157-165
- 34. Gibbs DJ, Tedds HM, et al. "Oxygen-dependent proteolysis regulates the stability of angiosperm polycomb repressive complex 2 subunit VERNALIZATION 2." Nat Commun. 2018 Dec 21;9(1):5438 PMID: 30575749
- 35. Oladimeji PO, Wright WC, et al. "RNA interference screen identifies NAA10 as a regulator of PXR transcription." Biochem Pharmacol. 2018 Dec 16;160:92-109 PMID: 30566892
- 36. Karademir B, Sari G, et al. "Proteomic approach for understanding milder neurotoxicity of Carfilzomib against Bortezomib." Sci Rep.2018 Nov 5;8(1):16318 PMID: 30397214
- 37. Xiang Y, Wang M, et al. "Mechanisms controlling the multistage post-translational processing of endogenous Nrf1α/TCF11 proteins to yield distinct isoforms within the coupled positive and negative feedback circuits." Toxicol Appl Pharmacol. 2018 Dec 1;360:212-235 PMID: 30287392
- 38. Rozic G, Paukov L, et al. "STK405759 as a combination therapy with bortezomib or dexamethasone, in in vitro and in vivo multiple myeloma models." Oncotarget. 2018 Jul 31;9(59):31367-31379 PMID: 30140376
- 39. Liew PL, Huang RL, et al. "Distinct methylation profile of mucinous ovarian carcinoma reveals susceptibility to proteasome inhibitors." Int J Cancer. 2018 Feb 16 PMID: 29451304
- 40. Farris TR, Zhu B, et al. "Ehrlichia chaffeensis TRP32 Nucleomodulin Function and Localization Is Regulated by NEDD4L-Mediated Ubiquitination." Front Cell Infect Microbiol. 2018 Jan 11;7:534 PMID: 29376035
- 41. Mañas A, Chen W, et al. "BaxΔ2 sensitizes colorectal cancer cells to proteasome inhibitor-induced cell death." Biochem Biophys Res Commun.2018 Jan 29;496(1):18-24 PMID: 29291406
- 42. Yuancai Xiang, et al. "Molecular mechanisms controlling the multistage post-translational processing of endogenous Nrf1α/TCF11 proteins to yield distinct proteoforms within the coupled positive and negative feedback circuits." bioRxiv.2018. April 12 10.1016/j.taap.2018.09.036
- 43. Yuancai Xiang, Josefin Halin, et al. "Topovectorial mechanisms control the juxtamembrane proteolytic processing of Nrf1 to remove its N-terminal polypeptides during maturation of the CNC-bZIP factor." bioRxiv.2018. March 27
- 44. Xinchun Li, Li Zhong, et al. "Phosphorylation of IRS4 by CK1γ2 promotes its degradation by CHIP through the ubiquitin/lysosome pathway." Theranostics, 2018, Vol. 8, Issue13
- 45. Ayse Tarbin Jannuzzi, Gulce Sari, et al. "Proteasomal Inhibition with Bortezomib Causes Selective Autophagy Upregulation and Perinuclear Clustering of Mitochondria in Human Neuronal Cells†." Proceedings 2018, 2(25), 1583
- 46. An H, Harper JW. "Systematic analysis of ribophagy in human cells reveals bystander flux during selective autophagy." Nat Cell Biol. 2017 Dec 11 PMID: 29230017
- 47. Chun H, Catterton T, et al. "Organ-specific regulation of ATP7A abundance is coordinated with systemic copper homeostasis." Sci Rep. 2017 Sep 20;7(1):12001 PMID: 28931909
- 48. Tian C, Yuan Z, et al. "Inhibition of glycolysis by a novel EGFR/HER2 inhibitor KU004 suppresses the growth of HER2+ cancer." Exp Cell Res. 2017 May 19. pii: S0014-4827(17)30297-5 PMID: 28532652
- 49. Rose CM, Isasa M, et al. "Highly Multiplexed Quantitative Mass Spectrometry Analysis of Ubiquitylomes." Cell Syst. 2016 Sep 21 PMID: 27667366
- 50. Le Goff X, Chesnel F, et al. "Aggregation dynamics and identification of aggregation-prone mutants of the von Hippel-Lindau tumor suppressor protein." J Cell Sci. 2016 Jul 1;129(13):2638-50 PMID: 27179072
- 51. Lee BH, Lu Y, et al. "USP14 deubiquitinates proteasome-bound substrates that are ubiquitinated at multiple sites." Nature. 2016 Apr 21;532(7599):398-401 PMID: 27074503
- 52. Moriwaki K, Chan FK. "Regulation of RIPK3- and RHIM-dependent Necroptosis by the Proteasome." J Biol Chem. 2016 Mar 11;291(11):5948-59 PMID: 26786097
- 53. Lai, Tsung-Hsuan, et al. "Gold Nanoparticles Compromise TNF-α-Induced Endothelial Cell Adhesion Molecule Expression Through NF-κB and Protein Degradation Pathways and Reduce Neointima Formation in a Rat Carotid Balloon Injury Model." Journal of Biomedical Nanotechnology 12.12 (2016): 2185-2201
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 384.24 |
| Cas No. | 179324-69-7 |
| Formula | C19H25BN4O4 |
| Synonyms | Bortezomib,PS-341,LDP-341,MLM341,MG-341,NSC-681239 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥19.21 mg/mL in DMSO |
| Chemical Name | [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid |
| Canonical SMILES | CC(C)C[C@@H](B(O)O)NC([C@H](Cc1ccccc1)NC(c1nccnc1)=O)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
| Cell lines | Canine malignant melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reaction Conditions | 72h; IC50=3.5~5.6 nM (nine kinds of cells) |
| Applications | Bortezomib potently suppressed the growth in 21 drugs, while other compounds had no or minimal effect on cell growth. We thus focused on bortezomib and examined its growth inhibitory properties against nine canine malignant melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML). Bortezomib inhibited the growth of all cell lines with calculated IC50 values of 3.5~5.6 nM. |
| Animal experiment [1]: | |
| Animal models | Nude athymic mice |
| Dosage form | 0.8 mg/kg; intravenous injection |
| Applications | The in vivo growth inhibitory activity of bortezomib against CMM-1 cells was evaluated using a xenograft mouse model. Bortezomib significantly suppressed the growth of tumours after Day 4 of treatment (P < 0.01, control vs. bortezomib). Tumours from the bortezomib-treated mice showed a significant decrease in mitotic index compared to controls (P |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Ito K, Kobayashi M, Kuroki S, et al. The proteasome inhibitor bortezomib inhibits the growth of canine malignant melanoma cells in vitro and in vivo[J]. The Veterinary Journal, 2013, 198(3): 577-582. | |
| Description | Bortezomib (PS-341) is a potent inhibitor of 20S proteasome with Ki of 0.6 nM. | |||||
| Targets | 20S proteasome | |||||
| IC50 | 0.6 nM (Ki) | |||||
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