Zetomipzomib maleate
Based on 4 publication(s) in Google Scholar
Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 2170983-62-5
- Formula: C34H46N4O12
- Molecular Weight:702.75
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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 maleate
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Biological Activity
Zetomipzomib maleate is an immunoproteasome-selective inhibitor[3]. Zetomipzomib maleate also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). Zetomipzomib maleate maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. Zetomipzomib maleate (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2170983-62-5
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Appearance Solid
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Molecular Weight 702.75
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Formula C34H46N4O12
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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.O=C(O)/C=C\C(O)=O
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Synonyms
KZR-616 maleate
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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 Sep 1;437(17):169229. PMID: 40414596 -
Curr Protoc
2024 Nov;4(11):e70057. PMID: 39574360
Solvent & Solubility
DMSO : 250 mg/mL (355.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (71.15 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.08 mg/mL (2.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (2.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (142.30 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (274 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)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [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 |
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| H2O / DMSO | 1 mM | 1.4230 mL | 7.1149 mL | 14.2298 mL | 35.5745 mL |
| 5 mM | 0.2846 mL | 1.4230 mL | 2.8460 mL | 7.1149 mL | |
| 10 mM | 0.1423 mL | 0.7115 mL | 1.4230 mL | 3.5575 mL | |
| 15 mM | 0.0949 mL | 0.4743 mL | 0.9487 mL | 2.3716 mL | |
| 20 mM | 0.0711 mL | 0.3557 mL | 0.7115 mL | 1.7787 mL | |
| 25 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.4230 mL | |
| 30 mM | 0.0474 mL | 0.2372 mL | 0.4743 mL | 1.1858 mL | |
| 40 mM | 0.0356 mL | 0.1779 mL | 0.3557 mL | 0.8894 mL | |
| 50 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7115 mL | |
| 60 mM | 0.0237 mL | 0.1186 mL | 0.2372 mL | 0.5929 mL | |
| DMSO | 80 mM | 0.0178 mL | 0.0889 mL | 0.1779 mL | 0.4447 mL |
| 100 mM | 0.0142 mL | 0.0711 mL | 0.1423 mL | 0.3557 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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