PF-3450074 (PF-74) exhibits anti-viral activities against HIV wild type NL4-3 and HIV T107N mutant with EC50 values of 0.72 μM and 4.5μM, respectively[1]. PF-3450074 (PF-74) displays a good potency in primary human peripheral blood mononuclear cells (PBMCs), inhibits HIV-193RW025, HIV-1JR-CSF and HIV-193MW965 with IC50 values of 1.5 ± 0.9 μM; 0.6 ± 0.20 μM; and 0.6 ± 0.10 μM, respectively. This compound shows Median IC50 and CC50 values of 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively[1]. The KD for the interaction between PF-74 and the CA hexamer, derived in the same manner as for NUP153, is determined to be 176 ± 78 nM[1]. PF-3450074 (PF-74) (10 μM; 8 hours) results in a marked reduction in late products of reverse transcription in HeLa-P4 cells with DNase I-treated stocks of Env-defective HIV-1 (R9.Env-)[2]. RT-PCR[2] Cell Line: HeLa-P4 cells Concentration: 10 μM Incubation Time: 8 hours Result: Inhibited HIV-1 reverse transcription in target cells.
Kinase Assay
Cell Assay
Animal Administration
References
[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.
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