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ONX-0914

Catalog No. T6029   CAS 960374-59-8
Synonyms: ONX0914, PR-957, ONX 0914

ONX-0914 (PR-957) is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome.

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ONX-0914 Chemical Structure
ONX-0914, CAS 960374-59-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
25 mg In stock $ 332.00
50 mg In stock $ 498.00
1 mL * 10 mM (in DMSO) In stock $ 157.00
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Purity: 99.31%
Purity: 98.47%
Purity: 98.35%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ONX-0914 (PR-957) is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome.
Targets&IC50 Immunoproteasome:~10 nM
In vitro 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.
In vivo In mouse models of rheumatoid arthritis and lupus, the maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight.
Kinase Assay 20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 μCi (γ)-32P ATP and 1.5 μM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.
Synonyms ONX0914, PR-957, ONX 0914
Molecular Weight 580.67
Formula C31H40N4O7
CAS No. 960374-59-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35 mg/mL

TargetMolReferences and Literature

1. Muchamuel T, et al. Nat Med, 2009, 15(7), 781-787.

TargetMolCitations

1. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326. 2. Guo T, Liu C, Yang C, et al. Immunoproteasome subunit PSMB8 regulates microglia-mediated neuroinflammation upon manganese exposure by PERK signaling. Food and Chemical Toxicology. 2022: 112951. 3. Li Y, Nan G, Hou X, et al.Non-peptidic immunoproteasome β5i-Selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification.European Journal of Medicinal Chemistry.2023: 115856.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library Anti-COVID-19 Compound Library Anti-Infection Compound Library Covalent Inhibitor Library Preclinical Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Anti-Bacterial Compound Library Ubiquitination Compound Library

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Keywords

ONX-0914 960374-59-8 Microbiology/Virology Proteases/Proteasome Ubiquitination Proteasome HIV Protease Antibacterial HIV Inhibitor ONX0914 inhibit PR-957 Bacterial PR957 PR 957 Human immunodeficiency virus ONX 0914 inhibitor

 

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