Pricing updated 2019-03-24. Prices are subject to change without notice.
Bortezomib is a dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM).1 It binds the β5-subunit of the 20S proteasome and selectively inhibits chymotryptic activity.2,3,4 In part by blocking the degradation of tumor-suppressing and proapoptotic proteins, bortezomib drives cell cycle arrest and apoptosis in cancer cell lines and has applications in multiple myeloma and certain lymphomas, as well as other types of cancer.1,5 Proteasome inhibitors, including bortezomib, have potential in combination therapy with chemotherapy and radiation therapy against cancer.6,7,8,9
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1. Ludwig, H., Khayat, D., Giaccone, G., et al. Proteasome inhibition and its clinical prospects in the treatment of hematologic and solid malignancies Cancer 104, 1794-1807 (2005).
2. Lightcap, E.S., McCormack, T.A., Pien, C.S., et al. Proteasome inhibition measurements: Clinical application Clinical Chemistry 46(5), 673-683 (2000).
Adams, J. Development of the proteasome inhibitor PS-
Dou, Q.P., and Zonder, J.A. Overview of proteasome inhibitor-
Richardson, P.G., Hideshima, T., and Anderson, K.C. Bortezomib (PS-
7. Minami, J., Suzuki, R., Mazitschek, R., et al. Histone deacetylase 3 (HDAC3) as a novel therapeutic target in multiple myeloma Leukemia 28(3), 680-689 (2014).
Mato, A.R., Feldman, T., and Goy, A. Proteasome inhibition and combination therapy for non-