Bortezomib-d8 (Synonyms: PS-341-d8; LDP-341-d8; NSC 681239-d8) |
| Catalog No.GC65010 |
보르테조밉-d8(PS-341-d8)은 보르테조밉으로 표시된 중수소입니다. 보르테조밉(PS-341)은 가역적이고 선택적인 프로테아좀 억제제이며 트레오닌 잔기를 표적으로 하여 20S 프로테아좀(Ki=0.6nM)을 강력하게 억제합니다. Bortezomib은 세포주기를 방해하고 세포 사멸을 유도하며 NF-κB를 억제합니다. 보르테조밉은 최초의 프로테아좀 억제제 항암제입니다. 항암 활성.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Bortezomib-d8 (PS-341-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].
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
[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.
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