2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. dBET57

dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1.

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dBET57 Chemical Structure

dBET57 Chemical Structure

CAS No. : 1883863-52-2

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Based on 2 publication(s) in Google Scholar

dBET57 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1[1][2].

IC50 & Target

BRD4 (BD1)

500 nM (DC50)

In Vitro

dBET57 (0-10000 nM, 72 h) inhibits the proliferation of NB cells, with the IC50 values for SK-N-BE(2), IMR-32, SH-SY5Y, HT22, HPAEC, 293T, HCAEC being 643.4, 299, 414, 2151, 2321, 4840 and 3939 nM[1].
dBET57 (0-1200 nM, 48 h) induces apoptosis in NB cells, and increases the proportion of cells in the G1 phase[1].
dBET57 (0-1200 nM, 0-48 h) reduces the migration and adhesion capabilities of NB cells[1].

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

dBET57 Related Antibodies

Cell Viability Assay[1]

Cell Line: SK-N-BE(2), IMR-32, SH-SY5Y, HT22, HPAEC, 293T, HCAEC
Concentration: 0-10000 nM
Incubation Time: 48 h
Result: Inhibited NB cell proliferation.

Western Blot Analysis[1]

Cell Line: SK-NBE(2), IMR-32, SH-SY5Y
Concentration: 0, 300, 600, 1200 nM
Incubation Time: 48 h
Result: Increased PARP activation in a dose-dependent manner, while Bcl-2 expression gradually decreased, reduced the expression of BRD4, BRD2, BRD3, and N-Myc.

Apoptosis Analysis[1]

Cell Line: SK-NBE(2), IMR-32, SH-SY5Y
Concentration: 0, 300, 600, 1200 nM
Incubation Time: 48 h
Result: Increased apoptosis rate in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: SK-NBE(2), IMR-32, SH-SY5Y
Concentration: 0, 300, 600, 1200 nM
Incubation Time: 72 h
Result: Increased the proportion of NB cells in G1 phase and decreased the proportion of NB cells in G2 and S phase.

Cell Migration Assay [1]

Cell Line: SK-NBE(2), IMR-32, SH-SY5Y
Concentration: 0, 1200 nM
Incubation Time: 48 h
Result: Reduced cell migration.
In Vivo

dBET57 (7.5 mg/kg, intraperitoneal injection, once daily, 2 weeks) has antitumor activity in the SK-NBE(2) xenograft mouse model[1].

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

Animal Model: SK-NBE(2) xenograft mouse model[1]
Dosage: 7.5 mg/kg, daily, 2 weeks
Administration: Intraperitoneal injection (i.p.)
Result: Reduced tumor volume, decreased the proportion of ki-67 positive cells, increased the proportion of caspase3, had no obvious organ toxicity, and downregulated the level of ZMYND8.
Molecular Weight

699.18

Formula

C34H31ClN8O5S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (357.56 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 1.4302 mL 7.1512 mL 14.3025 mL
5 mM 0.2860 mL 1.4302 mL 2.8605 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 (protect from light). 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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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (2.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 1.4302 mL 7.1512 mL 14.3025 mL 35.7562 mL
5 mM 0.2860 mL 1.4302 mL 2.8605 mL 7.1512 mL
10 mM 0.1430 mL 0.7151 mL 1.4302 mL 3.5756 mL
15 mM 0.0953 mL 0.4767 mL 0.9535 mL 2.3837 mL
20 mM 0.0715 mL 0.3576 mL 0.7151 mL 1.7878 mL
25 mM 0.0572 mL 0.2860 mL 0.5721 mL 1.4302 mL
30 mM 0.0477 mL 0.2384 mL 0.4767 mL 1.1919 mL
40 mM 0.0358 mL 0.1788 mL 0.3576 mL 0.8939 mL
50 mM 0.0286 mL 0.1430 mL 0.2860 mL 0.7151 mL
60 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5959 mL
80 mM 0.0179 mL 0.0894 mL 0.1788 mL 0.4470 mL
100 mM 0.0143 mL 0.0715 mL 0.1430 mL 0.3576 mL
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dBET57 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:

dBET571883863-52-2dBET 57dBET-57PROTACsEpigenetic Reader DomainApoptosisAnti-tumorBRD4Inhibitorinhibitorinhibit

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