2. Anti-infection
  3. HIV
  4. PF-3450074

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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PF-3450074 Chemical Structure

PF-3450074 Chemical Structure

CAS No. : 1352879-65-2

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Customer Review

Based on 3 publication(s) in Google Scholar

PF-3450074 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target[1]

HIV-1 (NL4.3 strain)

0.72 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
MT4 CC50
> 70.5 μM
Compound: PF-74
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
[PMID: 30243152]
MT4 CC50
145.18 μM
Compound: PF-74
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
[PMID: 32298111]
MT4 CC50
32.27 μM
Compound: PF74
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
[PMID: 34592608]
MT4 CC50
32.27 μM
Compound: PF74
Cytotoxicity against mock infected human MT4 cells by MTT assay
Cytotoxicity against mock infected human MT4 cells by MTT assay
[PMID: 34653770]
TZM CC50
> 23.5 μM
Compound: PF-74
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
[PMID: 32066010]
TZM CC50
> 47 μM
Compound: PF-74
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
[PMID: 32298111]
TZM CC50
> 50 μM
Compound: 1; PF74
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
[PMID: 35028563]
TZM CC50
76 μM
Compound: 1
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
[PMID: 32438252]
In Vitro

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.

PF-3450074 Related Antibodies

RT-PCR[2]

Cell Line: HeLa-P4 cells
Concentration: 10 μM
Incubation Time: 8 hours
Result: Inhibited HIV-1 reverse transcription in target cells.
Molecular Weight

425.52

Formula

C27H27N3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3501 mL 11.7503 mL 23.5007 mL
5 mM 0.4700 mL 2.3501 mL 4.7001 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 6.25 mg/mL (14.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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PF-3450074 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-34500741352879-65-2PF-74PF3450074PF 3450074PF74PF 74HIVHuman immunodeficiency viruscapsid proteinCAPBMCInhibitorinhibitorinhibit

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