Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 ( IC 50 : 39/57 nM=hLMP7/mLMP7) and LMP2 ( IC 50 : 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases.

Zetomipzomib maleate also inhibits MECL-1 subunit (IC 50 =623 nM) and constitutive proteasome β5 subunit (IC 50 =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]. Zetomipzomib maleate is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587)[3].

Zetomipzomib 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]. 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.

2170983-62-5

C34H46N4O12

702.758

KZR-616 maleate;Zetomipzomib maleate;Zetomipzomib maleate

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years