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ONX-0914

Cat. No. M2071

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ONX-0914 Structure
Synonym:

PR-957

Size Price Availability Quantity
1mg USD 60  USD60 In stock
2mg USD 100  USD100 In stock
5mg USD 150  USD150 In stock
10mg USD 237  USD237 In stock
25mg USD 475  USD475 In stock
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Quality Control & Documentation
Biological Activity

Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation.

Product Citations
Customer Product Validations & Biological Datas
Source Mol Cell Protomics (2016). Figure 4.ONX-0914 (Cat. No. M2071, Abmole Bioscience)
Method Immunoproteasome Activity Assays
Cell Lines
Concentrations 20μM
Incubation Time 60 min
Results Levels of ubiquitinated proteins in total homogenates and oxidized proteins in cytosolic homogenates (as determined using the OxyBlot procedure, which detects carbonylated proteins) were increased in I79N mice relative to WT and R278C mice, consistent with impaired UPS function.
Protocol (for reference only)
Cell Experiment
Cell lines ALL and AML cells
Preparation method MTT cytotoxicity assay Cytotoxicity of bortezomib, dexamethasone, as well as their combination, and carfilzomib, ONX 0912, ONX 0914, and 5AHQ was determined using the MTT colorimetric dye reduction assay. For the drug combination study, CalcuSyn (Version 1.1.1 1996, Biosoft, Cambridge, UK) software was used to calculate a combination index (CI) based on the median-effect principle, for each drug combination tested.
Concentrations 0~1µM
Incubation time 96h
Animal Experiment
Animal models RIP-GP mice model
Formulation an aqueous solution of 10% (wt/vol) sulfobutylether-b-cyclodextrin and 10 mM sodium citrate (pH 3.5)
Dosages 6 mg per kg body weight for 10 d
Administration a single i.v. bolus
Chemical Information
Molecular Weight 580.67
Formula C31H40N4O7
CAS Number 960374-59-8
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Basler M, et al. J Immunol. The antiviral immune response in mice devoid of immunoproteasome activity.

[2] Ichikawa HT, et al. Arthritis Rheum. Beneficial effect of novel proteasome inhibitors in murine lupus via dual inhibition of type I interferon and autoantibody-secreting cells.

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Keywords: ONX-0914, PR-957 supplier, Proteasome, inhibitors, activators

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