Zetomipzomib
Based on 4 publication(s) in Google Scholar
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 1629677-75-3
- Formula: C30H42N4O8
- Molecular Weight:586.68
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Storage:
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Zetomipzomib
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Biological Activity
Zetomipzomib also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). Zetomipzomib maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. Zetomipzomib (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1]. Zetomipzomib is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:7-8 week old female BALB/c mice (CAIA model)[1]
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Dosage:I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day
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Administration:5 mg/kg
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Result:Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model.
Chemical Information
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CAS No. 1629677-75-3
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Appearance Solid
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Molecular Weight 586.68
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Formula C30H42N4O8
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Color White to off-white
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SMILES
O=C(N[C@@H](CC1=CCCC1)C([C@]2(C)OC2)=O)[C@@H](NC([C@@H](NC(CN3CCOCC3)=O)C)=O)[C@H](O)C4=CC=C(OC)C=C4
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Synonyms
KZR-616
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
Enhancing antitumour response to proteasome inhibitors with inhibitors of insulin-degrading enzyme, a new molecular vulnerability in multiple myeloma. [Abstract]2026 Mar 19. PMID: 41852107 -
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 -
J Mol Biol
Immunoproteasome-specific Subunit Alterations as a Potential Therapeutic Target for Mitochondriopathies. [Abstract]2025 May 23:169229. PMID: 40414596 -
Curr Protoc
2024 Nov;4(11):e70057. PMID: 39574360
Solvent & Solubility
DMSO : ≥ 50 mg/mL (85.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (4.26 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 (4.26 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.
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.
Purity & Documentation
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Data Sheet (277 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]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl) [Content Brief]
[3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646. [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 | 1.7045 mL | 8.5225 mL | 17.0451 mL | 42.6127 mL |
| 5 mM | 0.3409 mL | 1.7045 mL | 3.4090 mL | 8.5225 mL | |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7045 mL | 4.2613 mL | |
| 15 mM | 0.1136 mL | 0.5682 mL | 1.1363 mL | 2.8408 mL | |
| 20 mM | 0.0852 mL | 0.4261 mL | 0.8523 mL | 2.1306 mL | |
| 25 mM | 0.0682 mL | 0.3409 mL | 0.6818 mL | 1.7045 mL | |
| 30 mM | 0.0568 mL | 0.2841 mL | 0.5682 mL | 1.4204 mL | |
| 40 mM | 0.0426 mL | 0.2131 mL | 0.4261 mL | 1.0653 mL | |
| 50 mM | 0.0341 mL | 0.1705 mL | 0.3409 mL | 0.8523 mL | |
| 60 mM | 0.0284 mL | 0.1420 mL | 0.2841 mL | 0.7102 mL | |
| 80 mM | 0.0213 mL | 0.1065 mL | 0.2131 mL | 0.5327 mL |
Zetomipzomib Related Classifications
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