PS-341

PS-341 is a specific, reversible and cell permeable dipeptide boronic acid inhibitor of the chymotrypsin-like activity of the proteasome (Ki=0.6nM). It inhibits proliferation of various tumor cell lines with nanomolar potency. Its commercial version was approved by the USFDA for the treatment of relapsed multiple myeloma. The typical concentrations for cell culture use are 1-20 µM. For in vitro use, the typical concentrations are 10-100 µM.

Additional Information

Product Name: PS-341
Also Known As: Bortezomib; VELCADE; PS341; MG-341; MG341; Pyz-Phe-boroLeu; CAS# 179324-69-7
Catalog No.: F1201
Size: 25 mg
Molecular Weight: 384.2 Da
Species: N/A
Source: Synthetic
Stock: Powder
Concentration: N/A
Quality Assurance: >98% by HPLC and NMR
Storage: Eligible for room temperature shipping. Store at -20°C upon receiving; protect from air and ligh
PDF Data Sheet: Download PDF datasheet, MSDS
NCBI RefSeq: N/A
Image(s): No
Shipping Method: Room temperature shipping
References: 1. Yi-He Ling et al. (2002) Mol Cancer Ther, 1:841-849
2. Adams J. (2002) The Oncologist, 7:9-16
3. Ling, Y., et al. (2003).Clin.Cancer Res.9,1145-1154
4. Chauhan, D., et al. (2005) Cancer Cell 8: 407-419
5. Dudek SA et al. (2010) J Virol. 84:9439-51

Details

PS-341 is a specific, reversible and cell permeable dipeptide boronic acid inhibitor of the chymotrypsin-like activity of the proteasome (Ki=0.6nM). It inhibits proliferation of various tumor cell lines with nanomolar potency. Its commercial version was approved by the USFDA for the treatment of relapsed multiple myeloma. The typical concentrations for cell culture use are 1-20 µM. For in vitro use, the typical concentrations are 10-100 µM.

Images
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100 nM bovine 26S proteasome (Cat. # A1200) was incubated with DMSO or with 10 µM PS-341 for 10 min at 37 °C in 20 mM Tris, pH 7.1, 50 mM NaCl, 2 mM ATP, 5 mM MgCl2, 2 mM bME and 10% glycerol. The proteasome was then diluted 10X into 50 µM SUC-LLVY-AMC (Cat. # G1100) in a buffer containing 20 mM Tris, pH 7.1, 2 mM bME. The released AMC fluorescence was monitored by a plate reader.


Equal amount of whole cell lysates prepared from DMSO (lane 1) or 20 μM PS-341 (lane 2)-treated HEK293T cells were separated by SDS-PAGE and immunoblotted with an anti-Ub antibody. Cells were treated with DMSO or PS-341 for 4 hours.