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  3. iBRD4-BD1

iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology.

For research use only. We do not sell to patients.

iBRD4-BD1 Chemical Structure

iBRD4-BD1 Chemical Structure

CAS No. : 2839318-17-9

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5 mg USD 825 In-stock
10 mg USD 1400 In-stock
25 mg USD 2590 In-stock
50 mg USD 3885 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of iBRD4-BD1:

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  • Purity & Documentation

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Description

iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology[1].

In Vitro

iBRD4-BD1 has affinity and selectivity for the BET-family BRD4-BD1 with an IC50 value of 12 nM[1].
iBRD4-BD1 has affinity and selectivity for the BET-family BRD4-BD2, BRD3-BD1, BRD3-BD2, BRD2-BD1 and BRD2-BD2 with IC50 values of 16 μM, 1.0 μM , 75 μM , 280 nM and 7.1 μM, respectively[1].
iBRD4-BD1 (0-50 μM; 72 h) has cytotoxicity with an EC50 value of 2.3 μM in MM.1S cells[1].

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

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 0-300 pM
Incubation Time: 1 h
Result: Prevented the denaturation of BRD4 in a dose-dependent manner and showed stabilization of BRD4 at concentrations above 3 nM.

Cell Cytotoxicity Assay[1]

Cell Line: MM.1S cells
Concentration: 0-50 μM
Incubation Time: 72 h
Result: Showed cytotoxicity with an EC50 value of 2.3 μM in MM.1S cells.
Molecular Weight

521.58

Formula

C29H30F3N5O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(C1=CC=C(C2=C(C3=CC=NC(OC4=CC(C(C)C)=CC=C4C)=N3)N(C5CCNCC5)C=N2)C=C1)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.73 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 1.9173 mL 9.5863 mL 19.1725 mL
5 mM 0.3835 mL 1.9173 mL 3.8345 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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: 2.5 mg/mL (4.79 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.79 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9173 mL 9.5863 mL 19.1725 mL 47.9313 mL
5 mM 0.3835 mL 1.9173 mL 3.8345 mL 9.5863 mL
10 mM 0.1917 mL 0.9586 mL 1.9173 mL 4.7931 mL
15 mM 0.1278 mL 0.6391 mL 1.2782 mL 3.1954 mL
20 mM 0.0959 mL 0.4793 mL 0.9586 mL 2.3966 mL
25 mM 0.0767 mL 0.3835 mL 0.7669 mL 1.9173 mL
30 mM 0.0639 mL 0.3195 mL 0.6391 mL 1.5977 mL
40 mM 0.0479 mL 0.2397 mL 0.4793 mL 1.1983 mL
50 mM 0.0383 mL 0.1917 mL 0.3835 mL 0.9586 mL
60 mM 0.0320 mL 0.1598 mL 0.3195 mL 0.7989 mL
80 mM 0.0240 mL 0.1198 mL 0.2397 mL 0.5991 mL
100 mM 0.0192 mL 0.0959 mL 0.1917 mL 0.4793 mL
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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.

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Product Name:
iBRD4-BD1
Cat. No.:
HY-151594
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