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ONX-0914 TFA
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ONX-0914 TFA图片
包装与价格:
包装价格(元)
10mM*1 mL电议
5mg电议
10mg电议

半岛bd体育手机客户端 介绍
ONX-0914 (PR-957) TFA 是选择性的低分子量多肽-7 (LMP7) 的抑制剂,LMP7 是免疫蛋白酶体的类糜蛋白酶亚单位。ONX-0914 TFA 阻断细胞因子的产生并减轻实验性关节炎的进展。ONX-0914 TFA 是分枝杆菌蛋白酶体的非竞争性不可逆抑制剂 (Ki=5.2 μM)。ONX-0914 TFA 通过 HSF-1 介导的 p-TEFb 活化激活潜伏的 HIV-1。
别名PR-957 TFA
分子式C33H41F3N4O9
分子量694.7
溶解度DMSO : 100 mg/mL (143.95 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1[1][2][3].

ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation[1].

ONX-0914 (2-10 mg/kg; i.v,; on days 4, 6 and 8) meliorates disease in mouse arthritis[1]. ONX-0914 (2, 6 and 10 mg per kg body weight on days 25, 27, 29, 31 and 33; i.v.) treatment also induced a rapid therapeutic response in the T and B cell-dependent CIA (collagen-induced arthritis) model[1].

[1]. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis [published correction appears in Nat Med. 2009 Nov;15(11):1333]. Nat Med. 2009;15(7):781-787. [2]. Ro?man K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020;25(6):1305. Published 2020 Mar 12. [3]. Lin J, et al. PR-957, a selective immunoproteasome inhibitor, reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1. Biochem Pharmacol. 2018;156:511-523.

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