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Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名:
KZR-616
- 库存:
货期:电询
- 供应商:
MedChemExpress LLC
- 规格:
电询
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Zetomipzomib
CAS No. : 1629677-75-3
MCE 国际站:Zetomipzomib
产品活性:Zetomipzomib (KZR-616) 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=hLMP7/mLMP7)。Zetomipzomib 用于多种自身免疫性疾病的潜力。
研究领域:Metabolic Enzyme/Protease
作用靶点:Proteasome
In Vitro: Zetomipzomib also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). Zetomipzomib maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. Zetomipzomib (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC).Zetomipzomib is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587).
In Vivo: Zetomipzomib (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.
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