| Name | ONX-0914 |
| Description | ONX-0914 (PR-957) is a potent and highly specific immunoproteasome inhibitor with minimal cross-reactivity to the constitutive proteasome. |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.44 mM), Sonication is recommended.
DMSO : 50 mg/mL (86.11 mM), Sonication is recommended.
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| Keywords | Proteasome | PR957 | PR 957 | ONX-0914 | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV Protease | HIV | Bacterial |
| Inhibitors Related | Neomycin sulfate | Stavudine | Emtricitabine | Ampicillin sodium | Doxycycline (hyclate) | Kanamycin sulfate | Sulfamethoxazole sodium | Lamivudine | Doxycycline | Isoeugenol | Dimethyl sulfoxide | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Bioactive Compound Library | Ubiquitination Compound Library | Hematonosis Compound Library | Anti-Viral Compound Library | Inhibitor Library | Anti-Bacterial Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Infection Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
