ONX-0914


CAS No. : 960374-59-8

(Synonyms: PR-957)

960374-59-8
Price and Availability of CAS No. : 960374-59-8
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Cat. No. : HY-13207
M.Wt: 580.67
Formula: C31H40N4O7
Purity: >98 %
Solubility: DMSO : ≥ 35 mg/mL
Introduction of 960374-59-8 :

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[1][2][3]. IC50 & Target: IC50: ~10 nM (LMP7)[1]. In Vitro: ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation[1]. In Vivo: 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].

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