KZR-616 maleate
Names
[ CAS No. ]:
2170983-62-5
[ Name ]:
KZR-616 maleate
Biological Activity
[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].
[Related Catalog]:
[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].
[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]. 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.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C34H46N4O12
[ Molecular Weight ]:
702.75