Cat. No.: HY-101838

dBET1

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker).

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Pureté: 98.96%
CAS No.: 1799711-21-9
Formule: C₃₈H₃₇ClN₈O₇S
Masse moléculaire:785.27

Stockage:

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

dBET1 Chemical Structure

CAS No.: 1799711-21-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker^[1]. (Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker).

IC₅₀ & Target

BRD4

430 nM (EC₅₀)

Cereblon

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	12.3 μM Compound: 1; dBET1	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HeLa	IC₅₀	16.06 μM Compound: 1; dBET1	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HepG2	IC₅₀	19.8 μM Compound: 1; dBET1	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HGC-27	IC₅₀	0.88 μM Compound: 1; dBET1	Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HN-6	IC₅₀	7.07 μM Compound: dBET1	Antiproliferative activity against human HN-6 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human HN-6 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34119833]
MCF7	IC₅₀	5.3 μM Compound: 1; dBET1	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
MM1.S	IC₅₀	0.141 μM Compound: dBET1	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MM1.S	IC₅₀	2469 nM Compound: 1; dBET1	Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay	[PMID: 37084596]
MOLM-13	IC₅₀	657 nM Compound: 4; dBET1	Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]
MOLM-13	IC₅₀	140 nM Compound: d-BET1	Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
MV4-11	IC₅₀	42 nM Compound: d-BET1	Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
MV4-11	IC₅₀	0.013 μM Compound: dBET1	Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MV4-11	IC₅₀	11.8 nM Compound: 1; dBET1	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay	[PMID: 37084596]
MV4-11	IC₅₀	6.1 nM Compound: dBET1	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo assay	[PMID: 37178483]
PC-3	EC₅₀	50 nM Compound: dBET-1	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability measured after 5 days by Cell-Titer glo assay Cytotoxicity against human PC-3 cells assessed as reduction in cell viability measured after 5 days by Cell-Titer glo assay	[PMID: 36577036]
RS4-11	IC₅₀	78.8 nM Compound: 4; dBET1	Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]
RS4-11	IC₅₀	79 nM Compound: d-BET1	Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]

In Vitro

Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC₅₀= 0.14 μM, compare to IC₅₀= 1.1 μM with JQ1)^[1].

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

In Vivo

Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count^[1].

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

Chemical Information

CAS No. 1799711-21-9
Appearance Solid
Masse moléculaire 785.27
Formule C₃₈H₃₇ClN₈O₇S
Color White to light yellow
SMILES

O=C(NCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (20)

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Nature

Chromatin remodelling drives immune cell-fibroblast communication in heart failure. [Abstract]

2024 Nov;635(8038):434-443. PMID: 39443808

dBET1 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Nov;635(8038):434-443. [Abstract]

Western blot analysis of liver tissue showed the expression of endogenous long and short BRD4 subtypes after treatment with a carrier or the small molecule BET protein degrader dBET1 (50 mg/kg).
Mol Cell

Cullin-RING ligases employ geometrically optimized catalytic partners for substrate targeting. [Abstract]

2024 Apr 4;84(7):1304-1320.e16. PMID: 38382526

dBET1 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2024 Apr 4;84(7):1304-1320.e16. [Abstract]

Representative Western blots show the protein levels shown in the model breast cancer cell line MDA-MB-468, which was treated with the PROTACs (dBET1: 500 nM; 2 h) or DMSO shown, and after ectopic expression of UBE2R1 or UBE2R2.
Cancer Res

BRD4 Levels Determine the Response of Human Lung Cancer Cells to BET Degraders That Potently Induce Apoptosis through Suppression of Mcl-1. [Abstract]

2020 Jun 1;80(11):2380-2393. PMID: 32156781

dBET1 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jun 1;80(11):2380-2393. [Abstract]

The cell lines shown were treated with DMSO, 100 nmol/L ZBC260, 500 nmol/L dBET1, or 1000 nmol/L JQ-1 for 24 or 48 hours, respectively. Annexin V/flow cytometry was used to detect the lysis of PARP and caspase in cell samples exposed to the drugs for 24 hours to assess apoptosis.

dBET1 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jun 1;80(11):2380-2393. [Abstract]

The cell lines shown were treated with DMSO, 100 nmol/L ZBC260, 500 nmol/L dBET1, or 1000 nmol/L JQ-1 for 24 or 48 hours, respectively. Western blotting was used to assess the lysis of PARP and caspase in cell samples exposed to the drugs for 24 hours to evaluate apoptosis.

dBET1 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jun 1;80(11):2380-2393. [Abstract]

Before adding 100 nmol/L ZBC260 or 500 nmol/L dBET1, H157 cells were pretreated with 5 μmol/L MG132 for 30 minutes. Four hours later, the cells were collected for the preparation of whole-cell protein lysis buffer.
Nat Commun

A proximity biotinylation-based approach to identify protein-E3 ligase interactions induced by PROTACs and molecular glues. [Abstract]

2022 Jan 10;13(1):183. PMID: 35013300
Nat Commun

Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer. [Abstract]

2021 Jul 21;12(1):4441. PMID: 34290255
Adv Sci (Weinh)

Discovery of SKP2-Recruiting PROTACs for Target Protein Degradation. [Abstract]

2026 Apr;13(20):e15159. PMID: 41637562
J Control Release

A dual PROTAC nanocarrier amplifies DNA damage and STING activation for cancer immunotherapy. [Abstract]

2025 Oct 2;388(Pt 1):114290. PMID: 41045969
J Med Chem

Alkyne Two-Phase Strategy: Rapid Generation of TK-285-Derived PROTACs as BRD4 Degraders. [Abstract]

2026 Mar 19. PMID: 41852276
Biochem Pharmacol

Momordin Ic suppresses breast cancer growth by targeting ACTL8‑dependent glutamine metabolism and PI3K/AKT/mTOR-MYC. [Abstract]

2026 May:247:117761. PMID: 41621692
Int J Mol Sci

BRD4 Mediates Transforming Growth Factor-β-Induced Smooth Muscle Cell Differentiation from Mesenchymal Progenitor Cells. [Abstract]

2025 Aug 21;26(16):8074. PMID: 40869394
Cancer Biol Ther

BRD4 PROTAC degrader MZ1 exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B genes. [Abstract]

2022 Dec 31;23(1):1-15. PMID: 36170346
Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
ACS Chem Biol

Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway. [Abstract]

2019 Oct 18;14(10):2215-2223. PMID: 31553577
ACS Pharmacol Transl Sci

General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex. [Abstract]

2021 Feb 26;4(2):941-952. PMID: 33860212
J Immunol

Proteolysis-Targeting Chimeras Enhance T Cell Bispecific Antibody-Driven T Cell Activation and Effector Function through Increased MHC Class I Antigen Presentation in Cancer Cells. [Abstract]

2021 Jul 15;207(2):493-504. PMID: 34215653
Cancer Chemother Pharmacol

An inhibitor of BRD4, GNE987, inhibits the growth of glioblastoma cells by targeting C-Myc and S100A16. [Abstract]

2022 Dec;90(6):431-444. PMID: 36224471
Biochem Biophys Res Commun

Accelerating PROTAC drug discovery: Establishing a relationship between ubiquitination and target protein degradation. [Abstract]

2022 Nov 5:628:68-75. PMID: 36084553
Hematology

BRD4 PROTAC degrader MZ1 exhibits anti-B-cell acute lymphoblastic leukemia effects via targeting CCND3. [Abstract]

2023 Dec;28(1):2247253. PMID: 37594294
Research Square Print

November 18th, 2022
Chemrxiv

Oct 12, 2021.

Solvant et solubilité

In Vitro:

DMSO : 43.33 mg/mL (55.18 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

1.2734 mL

6.3672 mL

12.7345 mL

5 mM

0.2547 mL

1.2734 mL

2.5469 mL

10 mM

0.1273 mL

0.6367 mL

1.2734 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% Corn Oil

Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[1]. Winter GE, et al. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015 Jun 19;348(6241):1376-81. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2734 mL	6.3672 mL	12.7345 mL	31.8362 mL
	5 mM	0.2547 mL	1.2734 mL	2.5469 mL	6.3672 mL
	10 mM	0.1273 mL	0.6367 mL	1.2734 mL	3.1836 mL
	15 mM	0.0849 mL	0.4245 mL	0.8490 mL	2.1224 mL
	20 mM	0.0637 mL	0.3184 mL	0.6367 mL	1.5918 mL
	25 mM	0.0509 mL	0.2547 mL	0.5094 mL	1.2734 mL
	30 mM	0.0424 mL	0.2122 mL	0.4245 mL	1.0612 mL
	40 mM	0.0318 mL	0.1592 mL	0.3184 mL	0.7959 mL
	50 mM	0.0255 mL	0.1273 mL	0.2547 mL	0.6367 mL

Keywords

dBET1

20 Cited Publications

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dBET1

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) dBET1

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform Epigenetic Reader Domain

Activité biologique

Chemical Information

Publications (20)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

dBET1

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) dBET1

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform Epigenetic Reader Domain

Activité biologique

Chemical Information

Publications (20)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

dBET1 Related Classifications

Cat. No.: HY-101838