Bortezomib

Research use only, not for human use.

Bortezomib (PS-341) is a?potent, selective, competitive, orally active Proteasome inhibitor with Ki of 0.6 nM for 20S Proteasome.

Bortezomib (PS-341) is a?potent, selective, competitive, orally active Proteasome inhibitor with Ki of 0.6 nM for 20S Proteasome; shows only modest activity toward serine and thiol proteases (cathepsin G, elastase, chymotrypsin Ki>300 nM); inhibits the TNFα-stimulated activation of NF-κB in primary HUVE cells (IC50=0.5 uM) by blocking the degradation of the inhibitor IκBα; exhibits anti-inflammatory effects in vivo.Blood Cancer Approved(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.Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines.Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines.The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells.Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3).(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.

Cell Cycle Analysis Cell Line:PC-3 cells Concentration:100 nM Incubation Time:8 hoursResult:Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.Apoptosis Analysis Cell Line:JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines) Concentration:5-100 nM Incubation Time:20 hours Result:The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).Western Blot Analysis Cell Line:wtp53 (Granta-519), mutp53 (Jeko) cells Concentration:20 nM Incubation Time:1, 2, 4, 6, 14 hours Result:Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).

Animal Model:Male nude mice (xenograft tumor model bearing PC-3 cells)Dosage:0.3, 1 mg/kg Administration:Intravenous injection; once weekly for 4 weeks Result:Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.

PS-341 | PS341 | PS 341

Proteasome/Ubiquitin

Proteasome

20Sproteasome

Cancer

Blood cancer

179324-69-7

384.2372

C19H25BN4O4

>98% (HPLC)

10 mM in DMSO

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

Boronic acid, B-[(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]-

(-20℃)

With Ice Pack

≥ 2 years