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ONX 0914
- PR 957
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C31H40N4O7
- MW: 580.67
Description
ONX 0914 (PR957) is a selective inhibitor of LMP7/β5i, the chymotrypsin-like catalytic subunit of the immunoproteasome. It blocks production of inflammatory cytokines including IL-23, TNFα and IL-6 and attenuates experimental arthritis progression in mouse models.
The immunoproteasome shapes antigen processing and inflammatory cytokine production in immune cells. ONX 0914 is relevant for autoimmune disease research, immunoproteasome selectivity studies and anti-inflammatory pharmacology.
Key Features
- Selective LMP7/β5i immunoproteasome inhibitor
- Suppresses IL-23, TNFα and IL-6 production
- Anti-inflammatory activity reported below maximum tolerated doses
- Active in experimental arthritis models
Applications
- Immunoproteasome activity assays
- Autoimmune inflammation research
- Cytokine production studies
- Arthritis and immune-cell model profiling
More Information
| Parent CAS No. | 960374-59-8 |
|---|---|
| Chemical Name | (S)-3-(4-methoxyphenyl)-N-((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide |
| SMILES | O1CCN(CC(=O)N[C@@H](C)C(=O)N[C@@H](CC2C=CC(OC)=CC=2)C(=O)N[C@@H](CC2C=CC=CC=2)C(=O)[C@@]2(OC2)C)CC1 |&1:8,13,26,36,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C31H40N4O7/c1-21(32-27(36)19-35-13-15-41-16-14-35)29(38)34-26(18-23-9-11-24(40-3)12-10-23)30(39)33-25(28(37)31(2)20-42-31)17-22-7-5-4-6-8-22/h4-12,21,25-26H,13-20H2,1-3H3,(H,32,36)(H,33,39)(H,34,38)/t21-,25-,26-,31+/m0/s1 |
| InChiKey | WQAVPPWWLLVGFK-VTNASVEKSA-N |
| CID | 23642227 |
| Short Description | Proteasome inhibitor |
References
- T. Muchamuel et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis. Nat. Med. 2009, 15, 781-788.
- S.E. Verbrugge et al. Inactivating PSMB5 Mutations and P-Glycoprotein (Multidrug Resistance-Associated Protein/ATP-Binding Cassette B1) Mediate Resistance to Proteasome Inhibitors: Ex Vivo Efficacy of (...). J. Pharmacol. Exp. Ther. 2012, 341, 174-182.
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