2. Epigenetics
  3. Epigenetic Reader Domain
  4. PFI-4

PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC50 of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions.

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PFI-4 Chemical Structure

PFI-4 Chemical Structure

CAS No. : 900305-37-5

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Customer Review

Based on 1 publication(s) in Google Scholar

PFI-4 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PFI-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC50 of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions[1][2].

IC50 & Target

IC50: 3.517 μM (BRPF2), >10 μM (BRD4 (1)), 0.172 μM (BRPF1B), >10 μM (TRIM24)[1].
In Vitro

PFI-4 (1.25 μM; 7 or 11 days) inhibits differentiation of human osteoclasts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PFI-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: Osteoclasts
Concentration: 1.25 µM
Incubation Time: 7 or 11 days
Result: Significantly reduces MMP9 secretion in osteoclasts.
Molecular Weight

380.44

Formula

C21H24N4O3
CAS No.
Appearance

Solid

Color

Light green to green

SMILES

O=C(NC1=C(N2CCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
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 : 26 mg/mL (68.34 mM; Need ultrasonic and warming; 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 2.6285 mL 13.1427 mL 26.2854 mL
5 mM 0.5257 mL 2.6285 mL 5.2571 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
=
Concentration
×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (2.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 2.6285 mL 13.1427 mL 26.2854 mL 65.7134 mL
5 mM 0.5257 mL 2.6285 mL 5.2571 mL 13.1427 mL
10 mM 0.2629 mL 1.3143 mL 2.6285 mL 6.5713 mL
15 mM 0.1752 mL 0.8762 mL 1.7524 mL 4.3809 mL
20 mM 0.1314 mL 0.6571 mL 1.3143 mL 3.2857 mL
25 mM 0.1051 mL 0.5257 mL 1.0514 mL 2.6285 mL
30 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1904 mL
40 mM 0.0657 mL 0.3286 mL 0.6571 mL 1.6428 mL
50 mM 0.0526 mL 0.2629 mL 0.5257 mL 1.3143 mL
60 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
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PFI-4 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:

PFI-4900305-37-5PFI4PFI 4Epigenetic Reader Domainbone lossosteolytic malignant bone lesionsosteoclastsInhibitorinhibitorinhibit

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