ONX-0914 TFA
Based on 26 publication(s) in Google Scholar
ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.87%
- 화학식: C33H41F3N4O9
- 분자량:694.70
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ONX-0914 TFA
More- Cell. 2025 Aug 21;188(17):4567-4585.e32. [Abstract]
- Mol Cancer. 2023 Dec 4;22(1):196. [Abstract]
- Adv Mater. 2025 Jul;37(30):e2420393. [Abstract]
- Autophagy. 2025 Jun;21(6):1212-1227. [Abstract]
- Redox Biol. 2021 Nov:47:102167. [Abstract]
- Cell Death Dis. 2022 Oct 8;13(10):860. [Abstract]
- J Neuroinflammation. 2024 Aug 2;21(1):191. [Abstract]
- J Med Chem. 2025 Dec 25;68(24):26405-26417. [Abstract]
- Eur J Med Chem. 2021 Jul 5:219:113455. [Abstract]
- Biochem Pharmacol. 2020 Jul:177:113964. [Abstract]
- Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]
- Cells. 2021 Dec 6;10(12):3431. [Abstract]
- Int Immunopharmacol. 2020 Mar 3;82:106259. [Abstract]
- Am J Physiol Cell Physiol. 2025 Apr 16. [Abstract]
- Molecules. 2020 Mar 12;25(6):1305. [Abstract]
- Sci Rep. 2025 May 19;15(1):17284. [Abstract]
- Sci Rep. 2021 May 25;11(1):10883. [Abstract]
- Comput Struct Biotechnol J. 2023 Mar 28:21:2405-2418. [Abstract]
- Oncol Res. 2025 Aug 28;33(9):2573-2595. [Abstract]
- Neuroscience. 2023 Feb 1:510:82-94. [Abstract]
- Curr Protoc. 2025 Dec 13.
- Curr Protoc. 2024 Nov;4(11):e70057. [Abstract]
- Neuroreport. 2021 Oct 6;32(14):1206-1215. [Abstract]
- University of California, Irvine. 2026.
- bioRxiv. 2026 Mar 30:2026.03.28.714855. [Abstract]
- Evid Based Complement Alternat Med. 2021 Oct 12:2021:6426225. [Abstract]
Customer Validation & Images
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Biological Activity
제품 설명
IC50 & Target
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HIV-1 |
In Vitro
ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
ONX-0914 (2, 6 and 10 mg per kg body weight on days 25, 27, 29, 31 and 33; i.v.) treatment also induced a rapid therapeutic response in the T and B cell–dependent CIA (collagen-induced arthritis) model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Collagen antibody-induced arthritis (CAIA, Arthritis was induced in BALB/c mice with antibodies specific for type II collagen (mAb) and endotoxin)[1]
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Dosage:2, 6 or 10 mg per kg body weight
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Administration:I.v.; treated on days 4, 6 and 8
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Result:Blocked disease progression in a dose-dependent manner and completely ameliorated visible signs of disease at the highest dose.
Chemical Information
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Appearance Solid
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분자량 694.70
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화학식 C33H41F3N4O9
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Color White to off-white
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SMILES
O=C(N[C@@H](C)C(N[C@@H](CC1=CC=C(OC)C=C1)C(N[C@@H](CC2=CC=CC=C2)C([C@]3(C)OC3)=O)=O)=O)CN4CCOCC4.O=C(O)C(F)(F)F
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Synonyms
PR-957 TFA
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (26)
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Journal Impact Factor
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Most Recent
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Cell
The immunoproteasome disturbs neuronal metabolism and drives neurodegeneration in multiple sclerosis. [Abstract]2025 Aug 21;188(17):4567-4585.e32. PMID: 40532699 -
Mol Cancer
Immunoproteasome function maintains oncogenic gene expression in KMT2A-complex driven leukemia. [Abstract]2023 Dec 4;22(1):196. PMID: 38049829 -
Adv Mater
Differential Optical Imaging of Antigen Presentation Machinery Using Molecular Optical Reporters. [Abstract]2025 Jul;37(30):e2420393. PMID: 40370186 -
Autophagy
Limiting cap-dependent translation increases 20S proteasomal degradation and protects the proteomic integrity in autophagy-deficient skeletal muscle. [Abstract]2025 Jun;21(6):1212-1227. PMID: 39878121 -
Redox Biol
Deficient immunoproteasome assembly drives gain of α-synuclein pathology in Parkinson's disease. [Abstract]2021 Nov:47:102167. PMID: 34662812 -
Cell Death Dis
Inhibition of p38 MAPK or immunoproteasome overcomes resistance of chronic lymphocytic leukemia cells to Bcl-2 antagonist venetoclax. [Abstract]2022 Oct 8;13(10):860. PMID: 36209148 -
J Neuroinflammation
Targeting the immunoproteasome in hypothalamic neurons as a novel therapeutic strategy for high-fat diet-induced obesity and metabolic dysregulation. [Abstract]2024 Aug 2;21(1):191. PMID: 39095788 -
J Med Chem
α-Aminoboronic Acid Moieties in Boro Dipeptides Modulate Proteasome Subunit Selectivity and Provide Access to Compounds with Potent Anticancer and Anti-Inflammatory Activity. [Abstract]2025 Dec 25;68(24):26405-26417. PMID: 41344819 -
Eur J Med Chem
2021 Jul 5:219:113455. PMID: 33894528 -
Biochem Pharmacol
Immunoproteasome inhibitor DPLG3 attenuates experimental colitis by restraining NF-κB activation. [Abstract]2020 Jul:177:113964. PMID: 32278007 -
Biochem Pharmacol
PR-957, a selective immunoproteasome inhibitor, reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1. [Abstract]2018 Oct:156:511-523. PMID: 30170098
ONX-0914 TFA purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]
The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.
ONX-0914 TFA purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]
Western blot detection of the p-TEFb component CDK9, Cyclin T1 and CDK9 phosphorylation on Thr186, as well as its downstream RNA poly II CTD and phosphate CTD after J-Lat 10.6 cells are treated with PR-957 in dose-dependent manner.
ONX-0914 TFA purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]
J-Lat 10.6 cells are treated with DMSO, PR-957 (150 nM) or Carfilzomib (40 nM) alone with or without the HSF1 inhibitor KRIBB11 (1.25 µM) for 48 h. Then the cells are lysed, and Ser320 phosphorylated HSF1, total HSF1 and p24 are detected by Western blot with the corresponding antibodies.
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Cells
Fragment-Sized and Bidentate (Immuno)Proteasome Inhibitors Derived from Cysteine and Threonine Targeting Warheads. [Abstract]2021 Dec 6;10(12):3431. PMID: 34943940 -
Int Immunopharmacol
2020 Mar 3;82:106259. PMID: 32143000 -
Am J Physiol Cell Physiol
Immunoproteasome subunit PSMB8 promotes skeletal muscle regeneration by regulating macrophage phenotyping switch in mice. [Abstract]2025 Apr 16. PMID: 40241316 -
Molecules
2020 Mar 12;25(6):1305. PMID: 32178473 -
Sci Rep
Highly specific Immunoproteasome inhibitor M3258 induces proteotoxic stress and apoptosis in KMT2A::AFF1 driven acute lymphoblastic leukemia. [Abstract]2025 May 19;15(1):17284. PMID: 40389585 -
Sci Rep
Activity of immunoproteasome inhibitor ONX-0914 in acute lymphoblastic leukemia expressing MLL-AF4 fusion protein. [Abstract]2021 May 25;11(1):10883. PMID: 34035431 -
Comput Struct Biotechnol J
2023 Mar 28:21:2405-2418. PMID: 37066124 -
Oncol Res
Inhibition of Proteasome LMP2 Activity Suppresses Chil3 Expression in Mouse Colon Adenocarcinoma Tissue and Restrains Tumor Growth. [Abstract]2025 Aug 28;33(9):2573-2595. PMID: 40918453 -
Neuroscience
PR-957 Suppresses Th1 and Th17 Cell Differentiation via Inactivating PI3K/AKT Pathway in Alzheimer's Disease. [Abstract]2023 Feb 1:510:82-94. PMID: 36581132 -
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Curr Protoc
2024 Nov;4(11):e70057. PMID: 39574360 -
Neuroreport
Inhibition of immunoproteasome subunit low molecular mass polypeptide 7 with ONX-0914 improves hypoxic-ischemic brain damage via PI3K/Akt signaling. [Abstract]2021 Oct 6;32(14):1206-1215. PMID: 34406990 -
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bioRxiv
2026 Mar 30:2026.03.28.714855. PMID: 41959534 -
Evid Based Complement Alternat Med
Inhibition of the Immunoproteasome Subunit LMP7 Ameliorates Cerebral White Matter Demyelination Possibly via TGF β/Smad Signaling. [Abstract]2021 Oct 12:2021:6426225. PMID: 34675988
용액&용해도
In Vitro:
DMSO : 100 mg/mL (143.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis [published correction appears in Nat Med. 2009 Nov;15(11):1333]. Nat Med. 2009;15(7):781-787. [Content Brief]
[2]. Rožman K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020;25(6):1305. Published 2020 Mar 12. [Content Brief]
[3]. Lin J, et al. PR-957, a selective immunoproteasome inhibitor, reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1. Biochem Pharmacol. 2018;156:511-523. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4395 mL | 7.1974 mL | 14.3947 mL | 35.9868 mL |
| 5 mM | 0.2879 mL | 1.4395 mL | 2.8789 mL | 7.1974 mL | |
| 10 mM | 0.1439 mL | 0.7197 mL | 1.4395 mL | 3.5987 mL | |
| 15 mM | 0.0960 mL | 0.4798 mL | 0.9596 mL | 2.3991 mL | |
| 20 mM | 0.0720 mL | 0.3599 mL | 0.7197 mL | 1.7993 mL | |
| 25 mM | 0.0576 mL | 0.2879 mL | 0.5758 mL | 1.4395 mL | |
| 30 mM | 0.0480 mL | 0.2399 mL | 0.4798 mL | 1.1996 mL | |
| 40 mM | 0.0360 mL | 0.1799 mL | 0.3599 mL | 0.8997 mL | |
| 50 mM | 0.0288 mL | 0.1439 mL | 0.2879 mL | 0.7197 mL | |
| 60 mM | 0.0240 mL | 0.1200 mL | 0.2399 mL | 0.5998 mL | |
| 80 mM | 0.0180 mL | 0.0900 mL | 0.1799 mL | 0.4498 mL | |
| 100 mM | 0.0144 mL | 0.0720 mL | 0.1439 mL | 0.3599 mL |
ONX-0914 TFA Related Classifications
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