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Technical Data
| Formula | C31H40N4O7 |
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| Molecular Weight | 580.67 | CAS No. | 960374-59-8 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (172.21 mM) | |
| Water | 100 mg/mL (172.21 mM) | |||
| Ethanol | 100 mg/mL (172.21 mM) | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay. | ||
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| In vitro | ONX-0914 is 20- to 40-fold more selective for LMP7 over the next most sensitive sites, β5 or LMP2. ONX-0914 blocks presentation of LMP7-specific, MHC-I–restricted antigens in vitro and in vivo with minimal cross-reactivity for the constitutive proteasome. Selective inhibition of LMP7 by ONX-0914 blocks production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells. LMP7 inhibition blocks production of IL-23 by ~90% and of tumor necrosis factor-α (TNF-α) and IL-6 by ~50%.[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] | ||
| Features | The first highly selective, small molecule inhibitor of the immunoproteasome. Potential use in cancer and autoimmune diseases (e.g. rheumatoid arthritis, inflammatory bowel disease, and lupus). |
Protocol (from reference)
| Animal Study:[1] |
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Customer Product Validation
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Data from [Data independently produced by , , Cell Mol Bioeng, 2017, 10(2):174-185]
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Data from [Data independently produced by , , Parasite Immunol, 2015, 37(11):599-604.]
Selleck's ONX-0914 (PR-957) has been cited by 21 publications
| 20S constitutive proteasome, 20S immunoproteasome, and cathepsin S are high-sensitivity and independent markers of immunological activity in relapsing-remitting type of multiple sclerosis [ J Neurochem, 2024, 10.1111/jnc.16165] | PubMed: 38923513 |
| Impaired immunoproteasomal function exacerbates renal ischemia-reperfusion injury [ Exp Mol Pathol, 2024, 140:104939] | PubMed: 39426027 |
| Immunoproteasome subunit β5i promotes perifascicular muscle atrophy in dermatomyositis by upregulating RIG-I [ RMD Open, 2023, 9(1)e002818] | PubMed: 36854567 |
| Evaluation of Proteasome and Immunoproteasome Levels in Plasma and Peritoneal Fluid in Patients with Endometriosis [ Int J Mol Sci, 2023, 24(18)14363] | PubMed: 37762666 |
| Interferon-α promotes neo-antigen formation and preferential HLA-B-restricted antigen presentation in pancreatic β-cells [ bioRxiv, 2023, 2023.09.15.557918] | PubMed: 37745505 |
| Interferon-α promotes neo-antigen formation and preferential HLA-B-restricted antigen presentation in pancreatic β-cells [ bioRxiv, 2023, 2023.09.15.557918] | PubMed: 37745505 |
| Corilagin induces human glioblastoma U251 cell apoptosis by impeding activity of (immuno)proteasome [ Oncol Rep, 2021, 45(4)34] | PubMed: 33649855 |
| Efficiency of the four proteasome subtypes to degrade ubiquitinated or oxidized proteins [ Sci Rep, 2020, 10(1):15765] | PubMed: 32978409 |
| Short-Term ONX-0914 Administration: Performance and Muscle Phenotype in Mdx Mice [ Int J Environ Res Public Health, 2020, 17(14):E5211] | PubMed: 32707682 |
| Expression of the immunoproteasome subunit β5i in non-small cell lung carcinomas [ J Clin Pathol, 2020, jclinpath-2020-206618] | PubMed: 32943490 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.