Zetomipzomib (KZR-616) maleate 是首创的免疫蛋白酶体 (immunoproteasome) 抑制剂，选择性靶向免疫蛋白酶体亚基 LMP7 (IC₅₀: 39/57 nM=hLMP7/mLMP7) 和 LMP2 (IC₅₀: 131/179 nM=hLMP2/mLMP2)。Zetomipzomib maleate 用于多种自身免疫性疾病的潜力。

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.

Solid

Zetomipzomib maleate also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=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).
Zetomipzomib maleate is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587). has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143.
[2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Di

In Vitro: DMSO : 250 mg/mL (355.75 mM; Need ultrasonic)H₂O : 50 mg/mL (71.15 mM; Need ultrasonic)配制储备液