PF-3450074
Based on 5 publication(s) in Google Scholar
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. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
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- Purity: 98.89%
- CAS No.: 1352879-65-2
- 화학식: C27H27N3O2
- 분자량:425.52
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PF-3450074
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Biological Activity
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HIV-1 (NL4.3 strain) 0.72 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
>70.5 μM
Compound: PF-74
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 24 hrs by CytoTox-Glo cytotoxicity assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 24 hrs by CytoTox-Glo cytotoxicity assay
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[PMID: 30243152] |
| MT4 | CC50 |
145.18 μM
Compound: PF-74
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Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay
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[PMID: 32298111] |
| MT4 | CC50 |
32.27 μM
Compound: PF74
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
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[PMID: 34592608] |
| MT4 | CC50 |
32.27 μM
Compound: PF74
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Cytotoxicity against mock infected human MT4 cells by MTT assay
Cytotoxicity against mock infected human MT4 cells by MTT assay
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[PMID: 34653770] |
| TZM | CC50 |
>23.5 μM
Compound: PF-74
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Cytotoxicity against in human TZM-bl cells assessed as reduction in cell viability measured after 2 days by cell titre glo luminiscent cell viability assay
Cytotoxicity against in human TZM-bl cells assessed as reduction in cell viability measured after 2 days by cell titre glo luminiscent cell viability assay
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[PMID: 32066010] |
| TZM | CC50 |
>47 μM
Compound: PF-74
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Cytotoxicity in uninfected human TZM-bl assessed as reduction in cell viability incubated for 1 day by Cyto-tox-Glo cytotoxicity assay
Cytotoxicity in uninfected human TZM-bl assessed as reduction in cell viability incubated for 1 day by Cyto-tox-Glo cytotoxicity assay
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[PMID: 32298111] |
| TZM | CC50 |
>50 μM
Compound: 1; PF74
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Cytotoxicity against human TZM cells expressing GFP assessed as inhibition of cell growth incubated for 72 hrs by XTT assay
Cytotoxicity against human TZM cells expressing GFP assessed as inhibition of cell growth incubated for 72 hrs by XTT assay
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[PMID: 35028563] |
| TZM | CC50 |
76 μM
Compound: 1
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Cytotoxicity against human TZM-GFP cells incubated for 72 hrs by by XTT assay
Cytotoxicity against human TZM-GFP cells incubated for 72 hrs by by XTT assay
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[PMID: 32438252] |
| U-87MG ATCC | CC50 |
73 μM
Compound: PF-74
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Cytotoxicity against human U87 cells expressing CD4/CCR5
Cytotoxicity against human U87 cells expressing CD4/CCR5
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[PMID: 30243152] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa-P4 cells
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Concentration:10 μM
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Incubation Time:8 hours
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Result:Inhibited HIV-1 reverse transcription in target cells.
Chemical Information
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CAS No. 1352879-65-2
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Appearance Solid
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분자량 425.52
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화학식 C27H27N3O2
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Color Light yellow to yellow
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SMILES
O=C(N[C@@H](CC1=CC=CC=C1)C(N(C)C2=CC=CC=C2)=O)CC3=C(C)NC4=C3C=CC=C4
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Synonyms
PF-74
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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J Enzyme Inhib Med Chem
Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity. [Abstract]2025 Dec;40(1):2501743. PMID: 40371698 -
Metabolites
Metabolite Identification of HIV-1 Capsid Modulators PF74 and 11L in Human Liver Microsomes. [Abstract]2022 Aug 16;12(8):752. PMID: 36005624 -
Microbiol Spectr
A Broad-Spectrum Antiviral Molecule, Protoporphyrin IX, Acts as a Moderator of HIV-1 Capsid Assembly by Targeting the Capsid Hexamer. [Abstract]2023 Feb 14;11(1):e0266322. PMID: 36475726 -
bioRxiv
The host protein cyclophilin A inhibits HIV-1 nuclear entry by decreasing capsid elasticity. [Abstract]2025 Sep 3:2025.09.03.673798. PMID: 40950186 -
bioRxiv
2023 Nov 9:2023.11.08.566350. PMID: 37986899
용액&용해도
DMSO : 250 mg/mL (587.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3501 mL | 11.7503 mL | 23.5007 mL | 58.7516 mL |
| 5 mM | 0.4700 mL | 2.3501 mL | 4.7001 mL | 11.7503 mL | |
| 10 mM | 0.2350 mL | 1.1750 mL | 2.3501 mL | 5.8752 mL | |
| 15 mM | 0.1567 mL | 0.7834 mL | 1.5667 mL | 3.9168 mL | |
| 20 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9376 mL | |
| 25 mM | 0.0940 mL | 0.4700 mL | 0.9400 mL | 2.3501 mL | |
| 30 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9584 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4700 mL | 1.1750 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5875 mL |
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