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CAS No. :
MCE 国际站:ONX-0914 TFA
产品活性: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。
研究领域:Metabolic Enzyme/Protease | Anti-infection
作用靶点:Proteasome | Bacterial | HIV
In Vitro: ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation.
In Vivo: ONX-0914 (2-10 mg/kg; i.v,; on days 4, 6 and 8) meliorates disease in mouse arthritis.
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.
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