1. Metabolic Enzyme/Protease
  2. Proteasome
  3. KZR-616 maleate

KZR-616 maleate 

Cat. No.: HY-114419A
Handling Instructions

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=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases.

For research use only. We do not sell to patients.

KZR-616 maleate Chemical Structure

KZR-616 maleate Chemical Structure

CAS No. : 2170983-62-5

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Description

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=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases[1][2].

In Vitro

KZR-616 maleate also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].
KZR-616 maleate 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

KZR-616 maleate (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.
Molecular Weight

702.75

Formula

C₃₄H₄₆N₄O₁₂

CAS No.
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KZR-616 maleate
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