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ONX-0914

Chemical Structure : ONX-0914

CAS No.: 960374-59-8

ONX-0914 (PR-957, ONX0914, PR957)

Catalog No.: PC-43393Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
ONX-0914 (PR-957) 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.
ONX-0914 (PR-957) reverses signs of disease and results in reductions in cellular infiltration, cytokine production and autoantibody levels in experimental arthritis models.

Physicochemical Properties

M.Wt 580.6719
Formula C31H40N4O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 35 mg/mL

Chemical Name/SMILES

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

References

1. Muchamuel T, et al. Nat Med. 2009 Jul;15(7):781-7.

2. Basler M, et al. J Immunol. 2010 Jul 1;185(1):634-41.

3. Ichikawa HT, et al. Arthritis Rheum. 2012 Feb;64(2):493-503.

4. Verbrugge SE, et al. J Pharmacol Exp Ther. 2012 Apr;341(1):174-82.

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