| 产品描述： | ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 |
| 靶点： |
HIV-1 |
| 体外研究： |
ONX-0914 抑制 LMP7 特异性抗原呈递。ONX-0914 阻断小鼠脾细胞产生细胞因子并阻断 T 细胞分化 |
| 体内研究： |
ONX-0914 (2-10 mg/kg；静脉注射；在第 4、6 和 8 天) 改善小鼠关节炎的疾病。 ONX-0914 (第 2、6 和在第 25、27、29、31 和 33 天，每公斤体重 10 毫克；iv) 处理还在 T 和 B 细胞依赖性 CIA (胶原诱导的关节炎) 模型中诱导了快速处理反应。 Animal Model: Collagen antibody-induced arthritis (CAIA, Arthritis was induced in BALB/c mice with antibodies specific for type II collagen (mAb) and endotoxin) Dosage: 2, 6 or 10 mg per kg body weight Administration: I.v.; treated on days 4, 6 and 8 Result: Blocked disease progression in a dose-dependent manner and completely ameliorated visible signs of disease at the highest dose. |
| 参考文献： |
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. Rožman 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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.722 ml |
8.611 ml |
17.221 ml |
| 5 mM |
0.344 ml |
1.722 ml |
3.444 ml |
| 10 mM |
0.172 ml |
0.861 ml |
1.722 ml |
| 50 mM |
0.034 ml |
0.172 ml |
0.344 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京