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Chemical Structure : KZR-8445
Catalog No.: PC-20817Not For Human Use, Lab Use Only.
KZR-8445 (KZR8445) is a cyclic depsipeptide, client-selective Sec61 inhibitor with IC50 of 100 nM, targets the Sec61 translocon and selectively modulate Sec61-mediated protein biogenesis.
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KZR-8445 (KZR8445) is a cyclic depsipeptide, client-selective Sec61 inhibitor with IC50 of 100 nM, targets the Sec61 translocon and selectively modulate Sec61-mediated protein biogenesis.
KZR-8445 binds to the central region of the Sec61 lateral gate in an open configuration, with direct contacts to the lumenal plug.
KZR8445 blocks CoV-2 replication and virus-induced cytotoxicity in Vero cells, an effect that is likely mediated by inhibition of spike protein biogenesis.
KZR8445 could overcome dexamethasone resistance in T-cell acute lymphoblastic leukemia cells in vitro.
KZR-8445 potently inhibits the secretion of proinflammatory cytokines in primary immune cells and is highly efficacious in a mouse model of rheumatoid arthritis.
KZR-8445 binding stabilizes the lateral gate helices in a manner that traps select signal peptides in the Sec61 channel and prevents their movement into the lipid bilayer.
| M.Wt | 1083.97 | |
| Formula | C49H61BrF6N8O8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Shahid Rehan, et al. Nat Chem Biol. 2023 May 11. doi: 10.1038/s41589-023-01326-1.
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