ONX 0914 is a proteosome inhibitor known for treatming malignancies and more recently, effacaciously inducing apoptosis for cancers. Used in the treatment of autoimmune diseases.
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This potent protease inhibitor (FW = 580.67 g/mol; CAS 960374-59-8; Solubility: 100 mg/mL DMSO or H2O), also known as PR-957 and N-[2-(4- morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2- oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide, targets (IC50 = 10 nM) the chymotrypsin-like protease activity of immunoproteasomes, a distinct class of proteasome found mainly in monocytes and lymphocytes. These specialized proteasomes shape the antigenic repertoire presented on class I major histocompatibility complexes (MHC-I). ONX-0914 shows minimal cross-reactivity for the constitutive proteasome. Selective inhibition blocks production of Interleukin-23 (IL-23) by activated monocytes and interferon-γ and IL-2 by T cells.
