Molecular Formula | C27H27N3O2 |
Molar Mass | 425.52 |
Solubility | DMSO : 250 mg/mL (587.52 mM; Need ultrasonic) |
Appearance | powder |
Color | white to beige |
Storage Condition | 2-8°C |
Use | PF-3450074 (PF-74), a specific inhibitor of HIV-1 capsid protein (HIV-1 CA), showed broad-spectrum inhibition against HIV isolates, showing submicromolar titers (EC50=8-640 nM). PF-3450074 (PF-74), which acts in the early stages of HIV-1 infection, inhibits viral replication by direct competition with the binding of CPSF6 and NUP153 and blocks the removal, assembly and reverse transcription steps of the viral life cycle. CPSF6: nuclear host factor cleavage and polyadenylate-specific factor 6;NUP153: nuclear pore protein 153. |
Target | HIV-1 NL4.3 strain |
WGK Germany | 3 |
Reference Show more | 1: Xu JP, Francis AC, Meuser ME, Mankowski M, Ptak RG, Rashad AA, Melikyan GB, Cocklin S. 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. PubMed PMID: 30393786; PubMed Central PMCID: PMC6214487. 2: Saito A, Ferhadian D, Sowd GA, Serrao E, Shi J, Halambage UD, Teng S, Soto J, Siddiqui MA, Engelman AN, Aiken C, Yamashita M. Roles of Capsid-Interacting Host Factors in Multimodal Inhibition of HIV-1 by PF74. J Virol. 2016 May 27;90(12):5808-5823. doi: 10.1128/JVI.03116-15. Print 2016 Jun 15. PubMed PMID: 27076642; PubMed Central PMCID: PMC4886767. 3: Zhou J, Price AJ, Halambage UD, James LC, Aiken C. HIV-1 Resistance to the Capsid-Targeting Inhibitor PF74 Results in Altered Dependence on Host Factors Required for Virus Nuclear Entry. J Virol. 2015 Sep;89(17):9068-79. doi: 10.1128/JVI.00340-15. Epub 2015 Jun 24. PubMed PMID: 26109731; PubMed Central PMCID: PMC4524096. 4: Lad L, Clancy S, Koditek D, Wong MH, Jin D, Niedziela-Majka A, Papalia GA, Hung M, Yant S, Somoza JR, Hu E, Chou C, Tse W, Halcomb R, Sakowicz R, Pagratis N. Functional label-free assays for characterizing the in vitro mechanism of action of small molecule modulators of capsid assembly. Biochemistry. 2015 Apr 7;54(13):2240-8. doi: 10.1021/acs.biochem.5b00151. Epub 2015 Mar 24. PubMed PMID: 25774576. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.35 ml | 11.75 ml | 23.501 ml |
5 mM | 0.47 ml | 2.35 ml | 4.7 ml |
10 mM | 0.235 ml | 1.175 ml | 2.35 ml |
5 mM | 0.047 ml | 0.235 ml | 0.47 ml |