Art. -Nr.: HY-151593

dBRD4-BD1

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Based on 1 Customer Validation

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.
(Pink: BRD4 ligand (HY-151594); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W006445)).

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Reinheit: 98.02%
CAS. Nr.: 2839318-19-1
Formel: C₅₀H₅₃F₃N₈O₉
Molecular Weight:967.00

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

dBRD4-BD1 Chemical Structure

CAS. Nr.: 2839318-19-1

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Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1^[1]. (Pink: BRD4 ligand (HY-151594); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W006445)).

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Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 2839318-19-1
Appearance Solid
Molecular Weight 967.00
Formel C₅₀H₅₃F₃N₈O₉
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0341 mL

5.1706 mL

10.3413 mL

5 mM

0.2068 mL

1.0341 mL

2.0683 mL

10 mM

0.1034 mL

0.5171 mL

1.0341 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Divakaran A, et al. Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader. ACS Med Chem Lett. 2022 Sep 29;13(10):1621-1627. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dBRD4-BD1

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dBRD4-BD1 Related Classifications

HY-151593 Related Classifications