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ONX-0914

SKU: orb1223513

Description

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.

Images & Validation

Key Properties

CAS Number960374-59-8
MW580.6719
Purity>98% (HPLC)
FormulaC31H40N4O7
SMILESO=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
TargetProteasome
SolubilityDMSO: ≥ 35 mg/mL

Bioactivity

In Vivo
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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

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Protocol Information

ONX-0914 (orb1223513)

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Available Sizes

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100 mg
200 mg
500 mg
5 mg
$ 190.00
10 mg
$ 280.00
25 mg
$ 460.00
50 mg
$ 670.00