ONX-0914 | Immunoproteasome inhibitor

CAS:
 960374-59-8
Catalog Number:
 10-5885
ONX-0914 chemical structure

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ONX-0914 (960374-59-8) is a selective inhibitor of the LMP7 subunit of the immunoproteasome (IC50 = 65 nM for mouse) which is the chymotrypsin-like subunit.1 Treatment with ONX-0914 resulted in suppression of Th1 and Th17 cells but enhancement of regulatory T cell differentiation in mouse models of induced colitis.2 ONX-0914 retards rheumatoid arthritis progression3, ameliorates diabetic cardiomyopathy4 and attenuates atherosclerosis and metabolic syndrome in mice5.

References/Citations:

  1. Muchamuel et al. (2009), A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis; Nat. Med. 15 781
  2. Kalim et al. (2012), Immunoproteasome subunit LMP7 deficiency and inhibition suppresses Th1 and Th17 but enhances regulatory T cell differentiation; J. Immunol. 189 4182
  3. Qingyang et al. (2023), PR-957 retards rheumatoid arthritis progression and inflammation by inhibiting LMP7-mediated CD4+ T cell imbalance; Int. Immunopharmacol. 124 110860
  4. Wang et al. (2023), ONX0914 inhibition of immunoproteasome subunit LMP7 ameliorates diabetic cardiomyopathy via restraining endothelial-mesenchymal transition; Clin. Sci. (London) 137 1297
  5. Schaftenaar et al. (2024), Immunoproteasomal Inhibition With ONX-0914 Attenuates Atherosclerosis and Reduces White Adipose Tissue Mass and Metabolic Syndrome in Mice; Thromb. Vasc. Biol. 44 1346
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CAS:
960374-59-8
Catalog Number:
10-5885
Activity:
Immunoproteasome inhibitor
Chemical Names:
N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide
Alternate Name:
PR-957
Molecular Weight:
580.68
Molecular Formula:

C31H40N4O7

Solubility:
Soluble in DMSO (10 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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ONX-0914 (960374-59-8) is a selective inhibitor of the LMP7 subunit of the immunoproteasome (IC50 = 65 nM for mouse) which is the chymotrypsin-like subunit.1 Treatment with ONX-0914 resulted in suppression of Th1 and Th17 cells but enhancement of regulatory T cell differentiation in mouse models of induced colitis.2 ONX-0914 retards rheumatoid arthritis progression3, ameliorates diabetic cardiomyopathy4 and attenuates atherosclerosis and metabolic syndrome in mice5.

References/Citations:

  1. Muchamuel et al. (2009), A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis; Nat. Med. 15 781
  2. Kalim et al. (2012), Immunoproteasome subunit LMP7 deficiency and inhibition suppresses Th1 and Th17 but enhances regulatory T cell differentiation; J. Immunol. 189 4182
  3. Qingyang et al. (2023), PR-957 retards rheumatoid arthritis progression and inflammation by inhibiting LMP7-mediated CD4+ T cell imbalance; Int. Immunopharmacol. 124 110860
  4. Wang et al. (2023), ONX0914 inhibition of immunoproteasome subunit LMP7 ameliorates diabetic cardiomyopathy via restraining endothelial-mesenchymal transition; Clin. Sci. (London) 137 1297
  5. Schaftenaar et al. (2024), Immunoproteasomal Inhibition With ONX-0914 Attenuates Atherosclerosis and Reduces White Adipose Tissue Mass and Metabolic Syndrome in Mice; Thromb. Vasc. Biol. 44 1346

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