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 (K i =5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
性状
Solid
体外研究(In Vitro)
ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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]. Ro?man K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020;25(6):1305. Published 2020 Mar 12.
溶解度数据
In Vitro: DMSO : 100 mg/mL (143.95 mM; Need ultrasonic)配制储备液