2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. dBRD4-BD1

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.

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

dBRD4-BD1 Chemical Structure

dBRD4-BD1 Chemical Structure

CAS No. : 2839318-19-1

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Based on 1 publication(s) in Google Scholar

dBRD4-BD1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1[1].

In Vitro

dBRD4-BD1 (64 pM-25 nM; 24 h) degrades BDR4 in a dose-dependent manner[1].
dBRD4-BD1 (5 μM; 0-72 h) increases the protein level of BRD2 and BRD3[1].

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

dBRD4-BD1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 25, 5, 1, 0.2, 0.04, 0.008, 0.0016 nM and 320 pM, 64 pM
Incubation Time: 24 hours
Result: Degraded BDR4 in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 5 μM
Incubation Time: 0, 0.5, 1, 2, 4, 8, 12, 24, 30, 36, 48, 72 hours
Result: Increased the protein amount of BRD2 and BRD3 without decreasing cMyc protein level in 4 hr period.
Molecular Weight

967.00

Formula

C50H53F3N8O9
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCC(NCCOCCOCCN4CCC(CC4)N5C=NC(C6=CC=C(C(F)(F)F)C=C6)=C5C7=CC=NC(OC8=CC(C(C)C)=CC=C8C)=N7)=O)=CC=C3)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (103.41 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 1.0341 mL 5.1706 mL 10.3413 mL
5 mM 0.2068 mL 1.0341 mL 2.0683 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

×
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 (2.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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, 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 1.0341 mL 5.1706 mL 10.3413 mL 25.8532 mL
5 mM 0.2068 mL 1.0341 mL 2.0683 mL 5.1706 mL
10 mM 0.1034 mL 0.5171 mL 1.0341 mL 2.5853 mL
15 mM 0.0689 mL 0.3447 mL 0.6894 mL 1.7235 mL
20 mM 0.0517 mL 0.2585 mL 0.5171 mL 1.2927 mL
25 mM 0.0414 mL 0.2068 mL 0.4137 mL 1.0341 mL
30 mM 0.0345 mL 0.1724 mL 0.3447 mL 0.8618 mL
40 mM 0.0259 mL 0.1293 mL 0.2585 mL 0.6463 mL
50 mM 0.0207 mL 0.1034 mL 0.2068 mL 0.5171 mL
60 mM 0.0172 mL 0.0862 mL 0.1724 mL 0.4309 mL
80 mM 0.0129 mL 0.0646 mL 0.1293 mL 0.3232 mL
100 mM 0.0103 mL 0.0517 mL 0.1034 mL 0.2585 mL
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dBRD4-BD1 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:

dBRD4-BD12839318-19-1PROTACsEpigenetic Reader DomainBETselectivedurableInhibitorinhibitorinhibit

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