1. Metabolic Enzyme/Protease
  2. Proteasome
  3. Zetomipzomib

Zetomipzomib (Synonyms: KZR-616)

Cat. No.: HY-114419
Handling Instructions

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.

Zetomipzomib Chemical Structure

Zetomipzomib Chemical Structure

CAS No. : 1629677-75-3

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Description

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[1][2].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Zetomipzomib (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

586.68

Formula

C₃₀H₄₂N₄O₈

CAS No.
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