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

KZR-616 

Cat. No.: HY-114419
Handling Instructions

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. KZR-616 has the potential for multiple autoimmune diseases treatment.

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

KZR-616 Chemical Structure

KZR-616 Chemical Structure

CAS No. : 1629677-75-3

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Description

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. KZR-616 has the potential for multiple autoimmune diseases treatment[1][2].

In Vitro

KZR-616 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 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587)[3].

In Vivo

KZR-616 (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].

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

586.68

Formula

C₃₀H₄₂N₄O₈

CAS No.

1629677-75-3

SMILES

O=C(N[[email protected]@H](CC1=CCCC1)C([[email protected]]2(C)OC2)=O)[[email protected]@H](NC([[email protected]@H](NC(CN3CCOCC3)=O)C)=O)[[email protected]](O)C4=CC=C(OC)C=C4

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

KZR-616KZR616KZR 616Proteasomefirst-in-classselectiveimmunoproteasomeproteasomesubunitautoimmunearthritisCAIAPBMCInhibitorinhibitorinhibit

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KZR-616
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HY-114419
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