A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome
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ONX 0914

Item No. 16271

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(4-morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide
CAS Number
960374-59-8
Synonyms
  • PR-957
Molecular Formula
C31H40N4O7
Formula Weight
580.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlEthanol: 15 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
SMILES
O=C([C@]1(C)OC1)[C@@H](NC([C@H](CC2=CC=C(OC)C=C2)NC([C@H](C)NC(CN3CCOCC3)=O)=O)=O)CC4=CC=CC=C4
InChi Code
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
InChi Key
WQAVPPWWLLVGFK-VTNASVEKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $183

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    10 mg

    $297

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    25 mg

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    Product Description

    ONX 0914 is a selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human, respectively) and demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC50s = 0.92 and 1.04 µM for mouse and human, respectively).1,2 It can block the production of IL-23 by activated monocytes and the production of IFN-γ and IL-2 by T cells.1 ONX 0914 can also inhibit IL-17-producing T cells under TH17-polarizing conditions in vitro and reduce TH1 and TH17 cell differentiation in vivo.3 This compound has been shown to attenuate disease progression in several experimental models of autoimmune disorders as well as in some hematologic malignancies.1,4,5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Muchamuel, T., Basler, M., Aujay, M.A., et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis. Nat. Med. 15(7), 781-787 (2009).

    2. Huber, E.M., Basler, M., Schwab, R., et al. Immuno- and constitutive proteasome crystal structures reveal differences in substrate and inhibitor specificity. Cell 148(4), 727-738 (2012).

    3. Kalim, K.W., Basler, M., Kirk, C.J., et al. Immunoproteasome subunit LMP7 deficiency and inhibition suppresses Th1 and Th17 but enhances regulatory T cell differentiation. J. Immunol. 189(8), 4182-4193 (2012).

    4. Basler, M., Daiee, M., Moll, C., et al. Prevention of experimental colitis by a selective inhibitor of the immunoproteasome. J. Immunol. 185(1), 634-641 (2010).

    5. Niewerth, D., Franke, N.E., Jansen, G., et al. Higher ratio immune versus constitutive proteasome level as novel indicator of sensitivity of pediatric acute leukemia cells to proteasome inhibitors. Haematologica 98(12), 1896-1904 (2013).

    6. Niewerth, D., Kaspers, G.J., Assaraf, Y.G., et al. Interferon-γ-induced upregulation of immunoproteasome subunit assembly overcomes bortezomib resistance in human hematological cell lines. J. Hematol. Oncol. 7(1), 1-15 (2014).

    Product Citations

    Zerfas, B.L., Maresh, M.E., and Trader, D.J. The immunoproteasome: An emerging target in cancer and autoimmune and neurological disorders. J. Med. Chem. (2019).