Name: ONX-0914 (PR-957)
Price: 289.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    ONX-0914, previously known as PR-975, is a potent inhibitor of immunoproteasome, a form of proteasome generating peptides presented on major histocompatibility complex (MHC) class I molecule to cytotixic T cells, which selectively induces conformational changes in the S1 binding pocket of the immunoproteasome subunit β5i (low molecular mass polypeptide 7/LMP7) rather than the constitutive proteasome subunit β5 in human and mouse cells. ONX-0914 is able to block the production of proinflammatory cytokines from human peripheral blood mononuclear cells (PBMCs), activate mouse splenocytes, inhibit IL-17-producing T cells under TH17-polarizing cytokines in vitro, and attenuate disease progression of diabetes, arthritis, and colitis in mouse models.
- Properties
  - Alternative Name
    
    ONX-0914,PR-957; (2S)-3-(4-methoxyphenyl)-N-[(2S)-1-(2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide
    
    CAS Number
    
    960374-59-8
    
    Molecular Formula
    
    C31H40N4O7
    
    Molecular Weight
    
    580.67
    
    Purity
    
    96.55%
    
    Solubility
    
    ≥29.03 mg/mL in DMSO; insoluble in H2O; ≥69 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Kirby L, Jin J, et al. “Oligodendrocyte precursor cells present antigen and are cytotoxic targets in inflammatory demyelination." Nat Commun. 2019 Aug 29;10(1):3887. PMID:31467299
    2. Jimenez-Guarde?o JM, Apolonia L, et al. "Immunoproteasome activation enables human TRIM5α restriction of HIV-1." Nat Microbiol. 2019 Jun;4(6):933-940. PMID:30886358
    3.Leslie Kirby, Jing Jin, et al. "Oligodendrocyte Precursor Cells Are Co-Opted by the Immune System to Cross-Present Antigen and Mediate Cytotoxicity." bioRxiv. 2018 November 4.
    4. Dimasuay KG, Sanchez A, et al."Immunoproteasomes as a novel antiviral mechanism in rhinovirus-infected airways." Clin Sci (Lond). 2018 Aug 16;132(15):1711-1723. PMID:29980604
    5. Liu RT, Zhang P, et al. "ONX-0914, a selective inhibitor of immunoproteasome, ameliorates experimental autoimmune myasthenia gravis by modulating humoral response." J Neuroimmunol. 2017 Oct 15;311:71-78. PMID:28844501
    6. Ortega-Atienza S, Krawic C, et al. "20S immunoproteasomes remove formaldehyde-damaged cytoplasmic proteins suppressing caspase-independent cell death." Sci Rep. 2017 Apr 5;7(1):654. PMID:28381880
    7. Chen, S., et al. "Immunoproteasome dysfunction augments alternative polarization of alveolar macrophages." Cell Death & Differentiation (2016). PMID:26990663

ONX-0914 (PR-957)

ONX-0914 (PR-957)

Background

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