2377734-91-1
Chemical Structure
KZR-8445
- CAS 番号: 2377734-91-1
- Formula:C49H61BrF6N8O8
- Molecular Weight:1083.95
IUPAC Name: 3-((2R,5S,8S,11S,14S,17S,20S)-14-((1-(4-bromobenzyl)-1H-indol-3-yl)methyl)-8,17-diisobutyl-7,13,19,20-tetramethyl-3,6,9,12,15,18,21-heptaoxo-5,11-bis(2,2,2-trifluoroethyl)-1-oxa-4,7,10,13,16,19-hexaazacyclohenicosan-2-yl)propanenitrile
InChIKey: CGZVQQQJOKERIF-VJQXVDPDSA-N
SMILES: BrC(C=C1)=CC=C1CN2C3=CC=CC=C3C(C[C@@H]4N(C([C@@H](NC([C@@H](N(C([C@@H](NC([C@H](OC([C@@H](N(C([C@@H](NC4=O)CC(C)C)=O)C)C)=O)CCC#N)=O)CC(F)(F)F)=O)C)CC(C)C)=O)CC(F)(F)F)=O)C)=C2
Biological Activity: KZR-8445, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection[1].
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KZR-8445 | KZR-8445, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection. | |||||||||||||||||||||
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