ONX-0914ONX-0914
MedChemExpress (MCE)
HY-13207
960374-59-8
PR-957
99.72%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
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.
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].
HIV-1
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[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. [Content Brief]
[2]. Rožman K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020
25(6):1305. Published 2020 Mar 12. [Content Brief]
[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. [Content Brief]