| Bioactivity | 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]. |
| Target | Ki: 0.6 nM (20S proteasome) |
| Invitro | 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]. Cell Cycle Analysis[1] Cell Line: |
| In Vivo | Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice[1]. Animal Model: |
| Name | Bortezomib |
| CAS | 179324-69-7 |
| Formula | C19H25BN4O4 |
| Molar Mass | 384.24 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. |
Bortezomib
CAS: 179324-69-7 F: C19H25BN4O4 W: 384.24
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM)
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