| Field | Specification |
|---|---|
| Alternative names | KZR-616 maleate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C34H46N4O12 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Zetomipzomib maleate (KZR-616), a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50 39 nM and 57 nM for hLMP7 and mLMP7, respectively) and LMP2 (IC50 131 nM and 179 nM for hLMP2 and mLMP2, respectively) subunits of the immunoproteasome. It has potential for the research of multiple autoimmune diseases[1][2]. It is supplied as a white to off-white solid (C34H46N4O12, MW 702.75) at 99.84% purity.
Physical & Chemical Properties
| CAS Number | 2170983-62-5 |
|---|---|
| Molecular Formula | C34H46N4O12 |
| Molecular Weight | 702.75 g/mol |
| Purity | 99.84% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 250 mg/mL (355.75 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 50 mg/mL (71.15 mM; Requires sonication) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 250 mg/mL (355.75 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 50 mg/mL (71.15 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (2.96 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (2.96 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 3
| Composition | PBS |
|---|---|
| Result | 100 mg/mL (142.30 mM); clear solution; requires sonication |
Data provided by the manufacturer.
In Vitro
Zetomipzomib maleate acts as an immunoproteasome-selective inhibitor[3]. MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM) are also inhibited by Zetomipzomib maleate. In MOLT-4 cells, Zetomipzomib maleate retains selective inhibition of LMP7 and LMP2. In peripheral blood mononuclear cells (PBMC), Zetomipzomib maleate (250 nM) displays a cytokine inhibition profile that is comparable[1].
In Vivo
In the anticollagen antibody induced arthritis (CAIA) model, Zetomipzomib maleate (5 mg/kg; i.v.; dosing repeated on days 6, 8, 11, and 13) shows efficacy[1].
| Animal Model | 7-8 week old female BALB/c mice (CAIA model)[1] |
|---|---|
| Dosage | I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day |
| Administration | 5 mg/kg |
| Result | Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Enhancing antitumour response to proteasome inhibitors with inhibitors of insulin-degrading enzyme, a new molecular vulnerability in multiple myeloma. Br J Pharmacol 2026 Mar 19. PMID: 41852107
α-Aminoboronic Acid Moieties in Boro Dipeptides Modulate Proteasome Subunit Selectivity and Provide Access to Compounds with Potent Anticancer and Anti-Inflammatory Activity. J Med Chem 2025 Dec 25;68(24):26405-26417. PMID: 41344819
Immunoproteasome-specific Subunit Alterations as a Potential Therapeutic Target for Mitochondriopathies. J Mol Biol 2025 Sep 1;437(17):169229. PMID: 40414596
Synthesis and Application of a Caged Bioluminescent Probe for the Immunoproteasome. Curr Protoc 2024 Nov;4(11):e70057. PMID: 39574360
