Bortezomib

179324-69-7

C19H25BN4O4

DMSO : >= 83.3 mg/mL (216.79 mM)

Metabolic Enzyme/Protease; Apoptosis; Autophagy

Bortezomib (PS-341) is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib (PS-341) disrupts the cell cycle, induces apoptosis, and inhibits NF-kappaB. Bortezomib (PS-341) is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans^[1][2]. IC50 & Target: Ki: 0.6 nM (20S proteasome)^[1]
In Vitro: 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]. 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].