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.
Int. J. Mol. Sci. 2023 Oct 17;24(20), 15266.
Mitochondrial and Proteasome Dysfunction Occurs in the Hearts of Mice Treated with Triazine Herbicide Prometryn
ONX-0914 purchased from AbMole
Sci Rep. 2020 Feb 25;10(1):3386.
Gender-specific Changes in Energy Metabolism and Protein Degradation as Major Pathways Affected in Livers of Mice Treated With Ibuprofen
ONX-0914 purchased from AbMole
Mol Cell Proteomics. 2016 Mar 28.
Delineation of molecular pathways involved in cardiomyopathies caused by troponin T mutations.
ONX-0914 purchased from AbMole
2015 Mar.
Effects of the Ubiquitin Proteasome Inhibitor on Ion Channels in Left Ventricular Hypertrophy and Association of rs3807989 with Atrial Fibrillation
ONX-0914 purchased from AbMole
.jpg) |
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. |
| 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 |
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Proteasome Products |
|---|
| NIC-0102
NIC-0102 is an orally potent proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammasome activation.NIC-0102 showed potent anti-inflammatory effects in vivo in a DSS-induced ulcerative colitis model. In addition, NIC-0102 inhibited the production of pro-IL-1β. |
| Ac-WLA-AMC
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate. |
| Ac-Nle-Pro-Nle-Asp-AMC
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. |
| PR-39
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. |
| PSI
PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
