PF-3450074 (PF-74) 是 HIV-1 衣壳蛋白 (HIV-1 CA) 的特异性抑制剂，对 HIV 分离株表现出广谱抑制作用，显示出亚微摩尔级别的效价 (EC50=8-640 nM)。PF-3450074 (PF-74) 在 HIV-1 感染的早期阶段起作用，通过与 CPSF6 和 NUP153 的结合直接竞争来抑制病毒复制，并阻断病毒生命周期的脱膜，组装和逆转录步骤。CPSF6:核宿主因子裂解和聚腺苷酸特异性因子 6；NUP153:核孔蛋白 153。
货号:ajcx17062
CAS:1352879-65-2
分子式:C27H27N3O2
分子量：425.52
溶解度:DMSO: 250 mg/mL (587.52 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle[1][2]. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.

[1]. Xu JP, et al. Exploring Modifications of an HIV-1 Capsid Inhibitor: Design, Synthesis, and Mechanism of Action.J Drug Des Res. 2018;5(2). pii: 1070. Epub 2018 Aug 13. [2]. Shi J, et al. Small-molecule inhibition of human immunodeficiency virus type 1 infection by virus capsid destabilization.J Virol. 2011 Jan;85(1):542-9.