Product Description: Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].
Formula: C19H17D8BN4O4
References: [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. /[2]Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22./[3]Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24./[4]Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64./[5]Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9./[6]Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80./[7]Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18.
Molecular Weight: 392.29
Compound Purity: 98.0
Research Area: Cancer
Solubility: 10 mM in DMSO/DMSO : 50mg/mL (ultrasonic)/Ethanol : 66.67mg/mL (ultrasonic;warming;heat to 60°C)
Target: Apoptosis;Autophagy;NF-κB;Proteasome
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