BortezomibBortezomib
MedChemExpress (MCE)
HY-10227
179324-69-7
PS-341
LDP-341
NSC 681239
99.91%
4°C, protect from light *In solvent : -80°C, 6 months
-20°C, 1 month (protect from light)
Room temperature in continental US
may vary elsewhere.
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.
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].
Bortezomib (PS-341) (0.3-1 mg/kg
i.v.
once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice[1].
Ki: 0.6 nM (20S proteasome)[1] Cellular Effect Cell Line Type Value Description References
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59(11):2615-22. [Content Brief]
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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]