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Proteases/Proteasome Proteasome Bortezomib

Bortezomib

Catalog No. T2399   CAS 179324-69-7
Synonyms: Brotezamide, DPBA, LDP 341, MG 341, NSC 681239, Radiciol

Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay).

Bortezomib, CAS 179324-69-7
Pack Size Availability Price/USD Quantity
5 mg In stock 55.00
10 mg In stock 68.00
25 mg In stock 85.00
50 mg In stock 102.00
100 mg In stock 167.00
200 mg In stock 264.00
1 mL * 10 mM (in DMSO) In stock 55.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Preparing Solutions
Description Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay).
Targets&IC50 20S proteasome :ic50 0.6nM(Ki),  
Kinase Assay Inhibitors were synthesized and purified according to the procedures described in Adams et al.The inhibition constant (Ki) for each inhibitor was measured according to the method of Stein et al.using a fluorometric assay,monitoring peptide substrate cleavage of Z-Leu-Leu-Val-Tyr-amino methyl coumarin (Z = carbobenzyloxy) by the 20S proteasome [1].
Cell Research
The inhibitory effect of Bortezomib on cell growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-hour cultures are pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 μL of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer. (Only for Reference)
Cell lines: Human multiple myeloma cells line U266
Animal Research
Animal Model: Human plasmacytoma xenografts RPMI 8226
Synonyms Brotezamide , DPBA , LDP 341 , MG 341 , NSC 681239 , Radiciol
Purity 100.00%
Molecular Weight 384.24
Formula C19H25BN4O4
CAS No. 179324-69-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 71 mg/mL (184.8 mM)

Ethanol: Insoluble

Water: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

0.5% methylcellulose+0.2% Tween 80: 5 mg/mL

Citations

References and Literature
1. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22. 2. Boccadoro M, et al. Preclinical evaluation of the proteasome inhibitor bortezomib in cancer therapy. Cancer Cell Int. 2005 Jun 1;5(1):18. 3. Ling YH, et al. PS-341, a novel proteasome inhibitor, induces Bcl-2 phosphorylation and cleavage in association with G2-M phase arrest and apoptosis. Mol Cancer Ther. 2002 Aug;1(10):841-9. 4. LeBlanc R, et al. Proteasome inhibitor PS-341 inhibits human myeloma cell growth in vivo and prolongs survival in a murine model. Cancer Res. 2002 Sep 1;62(17):4996-5000.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Autophagy Compound Library Epigenetics Compound Library Protease Inhibitor Library Hematopoietic Toxicity Compound Library FDA-approved Drug Library Anti-cancer Approved drug Library Cardiotoxicity Compound Library Anti-Metabolism Disease Compound Library

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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.