ONX-0914

Research use only, not for human use.

ONX-0914 (PR-957) is a potent, selective inhibitor of the chymotrypsin-like subunit of immunoproteasome LMP7 with IC80 <100 nM.

ONX-0914 (PR-957) is a potent, selective inhibitor of the chymotrypsin-like subunit of immunoproteasome LMP7 with IC80 <100 nM, 20- to 40-fold more selective over β5 or LMP2; blocks presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo, blocks production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells; reverses signs of disease and results in reductions in cellular infiltration, cytokine production and autoantibody levels in experimental arthritis models.

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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.

PR-957 | ONX 0914 | ONX0914 | PR957 | PR 957

Proteasome/Ubiquitin

Proteasome

LMP7

Inflammation/Immunology

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960374-59-8

580.6719

C31H40N4O7

>98% (HPLC)

DMSO: ≥ 35 mg/mL

O=C(N[C@@H](CC1=CC=CC=C1)C([C@]2(C)OC2)=O)[C@@H](NC([C@@H](NC(CN3CCOCC3)=O)C)=O)CC4=CC=C(OC)C=C4

L-Tyrosinamide, N-[2-(4-morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years