[CAS NO. 960374-59-8] ONX-0914 (PR-957)
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PRODUCTS SPECIFICATIONS [960374-59-8]
Store
Catalog
SLK-S7172
Brand
Selleck
CAS
960374-59-8
DESCRIPTION [960374-59-8]
Overview
| MDL | MFCD26794217 |
|---|---|
| Molecular Weight | 580.67 |
| Molecular Formula | C31H40N4O7 |
| SMILES | O=C(N[C@@H](CC1=CC=CC=C1)C([C@]2(C)OC2)=O)[C@@H](NC([C@@H](NC(CN3CCOCC3)=O)C)=O)CC4=CC=C(OC)C=C4 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7221 mL | 8.6107 mL | 17.2215 mL |
| 5 mM | 0.3444 mL | 1.7221 mL | 3.4443 mL |
| 10 mM | 0.1722 mL | 0.8611 mL | 1.7221 mL |
| 50 mM | 0.0344 mL | 0.1722 mL | 0.3444 mL |
Description
ONX-0914 (PR-957) is a potent and selective inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay.
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).
Targets
| LMP7 [1] (Cell-free assay) |
| ~10 nM |
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%.
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%.
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