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PF-3450074

Catalog No. T16500 CAS 1352879-65-2

Synonyms: PF-74

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

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PF-3450074, CAS 1352879-65-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 133.00
50 mg	In stock	$ 226.00
100 mg	In stock	$ 397.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.92%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-3450074 (PF-74) acts at an early stage of HIV-1 infection inhibits viral replication by directly competing with the binding of CPSF6 (nuclear host factors cleavage and polyadenylation specific factor 6) and NUP153 (nucleoporin 153), and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. PF-3450074 is a specifical inhibitor of HIV-1 capsid protein (CA) and shows a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM).
Targets&IC50	HIV-1:0.72 μM(NL4.3 strain)
In vitro	PF-3450074 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. PF-3450074 shows anti-viral activities against HIV wild type NL4-3 and HIV T107N mutant (EC50: 0.72 μM and 4.5μM, respectively). PF-3450074 (10 μM; 8 hours) causes 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-). This compound shows Median IC50?and CC50?values of 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively. 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][2].
Cell Research	HeLa-P4 cells were inoculated with PF74 (10 μM). After 8 h of culture, the cells were harvested and DNA isolated with a DNeasy Blood & Tissue kit (Qiagen). HIV-1 DNA in the samples was quantified by real-time PCR using primers specific which shows that PF74 inhibited HIV-1 reverse transcription in target cells.

Synonyms	PF-74
Molecular Weight	425.52
Formula	C27H27N3O2
CAS No.	1352879-65-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 249 mg/mL (585.16 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Viral Compound Library Anti-Infection Compound Library

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Keywords

PF-3450074 1352879-65-2 Microbiology/Virology Proteases/Proteasome HIV Protease capsid protein inhibit PF 3450074 PF-74 PBMC PF74 Human immunodeficiency virus Inhibitor PF3450074 PF 74 HIV inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.