ONX-0914 (PR-957)
Modify Date: 2025-08-22 19:35:06
ONX-0914 (PR-957) structure
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Common Name | ONX-0914 (PR-957) | ||
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| CAS Number | 960374-59-8 | Molecular Weight | 580.672 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 878.0±65.0 °C at 760 mmHg | |
| Molecular Formula | C31H40N4O7 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 484.8±34.3 °C | |
Use of ONX-0914 (PR-957)ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.IC50 Value: ~10 nM [1]in vitro: PR-957 blocked presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo. Selective inhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells [1].in vivo: In mouse models of rheumatoid arthritis and lupus, ONX-0914 treatment reverses signs of disease and results in reductions in cellular infiltration, cytokine production and autoantibody levels at well-tolerated doses. The maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight. IFN-g release is inhibited by ~60% at LMP7-selective concentrations of ONX-0914 and by ~90% at higher concentrations. Production of IL-2 is also inhibited by ~50% [1]. |
| Name | (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 |
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| Synonym | More Synonyms |
| Description | ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.IC50 Value: ~10 nM [1]in vitro: PR-957 blocked presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo. Selective inhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells [1].in vivo: In mouse models of rheumatoid arthritis and lupus, ONX-0914 treatment reverses signs of disease and results in reductions in cellular infiltration, cytokine production and autoantibody levels at well-tolerated doses. The maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight. IFN-g release is inhibited by ~60% at LMP7-selective concentrations of ONX-0914 and by ~90% at higher concentrations. Production of IL-2 is also inhibited by ~50% [1]. |
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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 878.0±65.0 °C at 760 mmHg |
| Molecular Formula | C31H40N4O7 |
| Molecular Weight | 580.672 |
| Flash Point | 484.8±34.3 °C |
| Exact Mass | 580.289673 |
| PSA | 149.07000 |
| LogP | 3.41 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.569 |
| InChIKey | WQAVPPWWLLVGFK-UHFFFAOYSA-N |
| SMILES | COc1ccc(CC(NC(=O)C(C)NC(=O)CN2CCOCC2)C(=O)NC(Cc2ccccc2)C(=O)C2(C)CO2)cc1 |
| Storage condition | 2-8°C |
| qc-7242 |
| D-erythro-3-Pentulose, 4,5-anhydro-1,2-dideoxy-4-C-methyl-2-[[N-[2-(4-morpholinyl)acetyl]-L-alanyl-O-methyl-L-tyrosyl]amino]-1-phenyl- |
| 4,5-Anhydro-1,2-dideoxy-4-methyl-2-{[N-(4-morpholinylacetyl)-L-alanyl-O-methyl-L-tyrosyl]amino}-1-phenyl-D-erythro-pent-3-ulose |
| ONX-0914 |
| ONX0914 |