Zetomipzomib
CAS No. : 1629677-75-3
(Synonyms: KZR-616)
| Size | Price | Stock |
|---|---|---|
| 1mg | $818 | In-stock |
| 5mg | $1800 | In-stock |
| 10mg | $2850 | In-stock |
| 25mg | $5800 | In-stock |
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| Cat. No. : | HY-114419 |
| M.Wt: | 586.68 |
| Formula: | C30H42N4O8 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases[1][2]. 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)[1]. Zetomipzomib is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587)[3]. 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[1].
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