Zetomipzomib maleate

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=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases. In Vitro Zetomipzomib maleate is an immunoproteasome-selective inhibitor. 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). ? MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . 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) 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. Form:Solid

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