Bortezomib

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) [1][2]. Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) [7].

Product Specifications

CAS Number

[179324-69-7]

Product Name Alternative

PS-341; LDP-341; NSC 681239

UNSPSC

12352005

Hazard Statement

H303, H315, H319, H361, H373

Target

Apoptosis; Autophagy; NF-κB; Proteasome; TREM receptor

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Bortezomib.html

Purity

99.97

Solubility

DMSO : 50 mg/mL (ultrasonic) |Ethanol : 66.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O

Molecular Formula

C19H25BN4O4

Molecular Weight

384.24

Precautions

H303, H315, H319, H361, H373

References & Citations

[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.|[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.