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首页-小分子抑制剂&激动剂-Others-Other Targets-KZR-8445
KZR-8445

Chemical Structure : KZR-8445

CAS No.: 2377734-91-1

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KZR-8445 (KZR8445)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 1083.97
分子式 C49H61BrF6N8O8
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

CC(C)C[C@H](NC1=O)C(N([C@H](C(O[C@@H](C(N[C@@H](CC(F)(F)F)C(N(C)[C@H](C(N[C@H](C(N(C)[C@H]1CC2=CN(CC3=CC=C(Br)C=C3)C4=C2C=CC=C4)=O)CC(F)(F)F)=O)CC(C)C)=O)=O)CCC#N)=O)C)C)=O

参考文献

1. Shahid Rehan, et al. Nat Chem Biol. 2023 May 11. doi: 10.1038/s41589-023-01326-1.

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