Bortezomib

SKU: orb1225902

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 179324-69-7
• MW: 384.2372
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₅BN₄O₄
• SMILES: CC(C)C[C@@H](B(O)O)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O
• Target: Proteasome
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.
• In Vitro:
  Cell Cycle Analysis Cell line: PC-3 cells. Concentration: 100 nM. Incubation time: 8 hours. Result: 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PS-341 | PS341 | PS 341

Quick Database Links

Gene Symbol

Proteasome