Art. -Nr.: HY-112588

dBET6

40 Cited Publications

Kundenbewertung

Based on 40 publication(s) in Google Scholar

dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 14 nM, and has antitumor activity.
(Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-103596); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.90%
CAS. Nr.: 1950634-92-0
Formel: C₄₂H₄₅ClN₈O₇S
Molecular Weight:841.37

Speicherung:

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

dBET6 Chemical Structure

CAS. Nr.: 1950634-92-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (40)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 14 nM, and has antitumor activity. (Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-103596); Black: linker).

IC₅₀ & Target^[1]

BET

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	10.33 nM Compound: dBET6	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay	[PMID: 35395439]

In Vitro

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC₅₀ of 14 nM. dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4^[1].

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

In Vivo

dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL^[1].

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

Chemical Information

CAS. Nr. 1950634-92-0
Appearance Solid
Molecular Weight 841.37
Formel C₄₂H₄₅ClN₈O₇S
Color White to light yellow
SMILES

O=C(NCCCCCCCCNC(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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (40)

All OthersBio/Physico-chemical AssayWBFlow CytometryCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Immunol

Mechanism for controlled assembly of transcriptional condensates by Aire. [Abstract]

2024 Sep;25(9):1580-1592. PMID: 39169234
Mol Cell

A BRD4-mediated elongation control point primes transcribing RNA polymerase II for 3'-processing and termination. [Abstract]

2021 Sep 2;81(17):3589-3603.e13. PMID: 34324863

dBET6 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 Sep 2;81(17):3589-3603.e13. [Abstract]

Total RNA level changes (log2 fold-changes) upon 2 h (top panel) and 6 h (lower panel) of dBET6 (100 nM) treatment in MOLT4 cells. Significant (FDR <0.05) down- and up-regulated genes are in blue and red, respectively. The data were RLE normalized to the spiked-in ERCC mix.
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Intrinsic signaling pathways modulate targeted protein degradation. [Abstract]

2024 Jul 2;15(1):5379. PMID: 38956052

dBET6 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 2;15(1):5379. [Abstract]

HiBiT-BRD4 cells were treated with PDD, GSK, or luminespib (1, 3, or 10 μM) for 4 h and with 50 nM dBET6 for 2 h (n =3, biological replicates). The results demonstrate that the aforementioned compounds promote BRD4 degradation induced by the CRL4^CRBN-based degrader dBET6.
Nat Commun

Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation. [Abstract]

2024 Jun 26;15(1):5409. PMID: 38926334
Nat Commun

Delivery of a BET protein degrader via a CEACAM6-targeted antibody-drug conjugate inhibits tumour growth in pancreatic cancer models. [Abstract]

2024 Mar 11;15(1):2192. PMID: 38467634
Nat Chem Biol

Template-assisted covalent modification underlies activity of covalent molecular glues. [Abstract]

2024 Dec;20(12):1640-1649. PMID: 39075252

dBET6 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1640-1649. [Abstract]

Western blot of BRD4 degradation in K562 cells that were treated with DMSO or different concentrations of MMH1, MMH2, dBET6 (1-100 nM) or MZ1 for 6 h.

dBET6 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1640-1649. [Abstract]

Flow cytometry analysis of BRD4_BD2-eGFP degradation in K562 cells that were treated with increasing concentrations of MMH1, MMH2, dBET6 or MZ1 for 2 h, 6 h, or 16 h (n = 3).
Nat Chem Biol

Activity-based profiling of cullin-RING E3 networks by conformation-specific probes. [Abstract]

2023 Dec;19(12):1513-1523. PMID: 37653169
Nat Chem Biol

Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders. [Abstract]

2023 Mar;19(3):323-333. PMID: 36329119

dBET6 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Mar;19(3):323-333. [Abstract]

Protein levels in RKO CRBN-/- cells with over-expression of CRBNWT, CRBNN351D, CRBNH397D or CRBNH57D treated with DMSO, CC-90009 (50 nM, 6 h), dBET6 (15 nM, 2 h), dBET57 (240 nM, 2 h) or THAL-SNS-032 (200 nM, 2 h).

dBET6 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Mar;19(3):323-333. [Abstract]

Depiction of clonogenic assays via crystal violet staining. Cells were treated for 10 days at EC90 of the degrader (30 nM dBET6, 60 nM CC-90009).
Blood Cancer Discov

Rapid Transcription Dynamics Confers Cytarabine Resistance in Acute Myeloid Leukemia. [Abstract]

2026 Jul 1;7(4):624-641. PMID: 42149820
Cell Rep Med

A triple-action PROTAC for wild-type p53 cancer therapy. [Abstract]

2025 Dec 16;6(12):102467. PMID: 41308642
Clin Cancer Res

CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]

2024 Sep 13;30(18):4179-4189. PMID: 39052240
Cell Genom

Pooled endogenous protein tagging and recruitment for systematic profiling of protein function. [Abstract]

2024 Sep 4:100651. PMID: 39255790
NPJ Precis Oncol

Targeting ACE2-BRD4 crosstalk in colorectal cancer and the deregulation of DNA repair and apoptosis. [Abstract]

2023 Feb 18;7(1):20. PMID: 36801948
J Med Chem

Real-Time NanoBRET Target Engagement Reveals Permeability-Activity Relationships in BET-Targeting Degraders. [Abstract]

2026 May 28;69(10):12669-12677. PMID: 42139371
J Med Chem

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

2026 Mar 19. PMID: 41852276
Cancers (Basel)

Deacetylase Plus Bromodomain Inhibition Downregulates ERCC2 and Suppresses the Growth of Metastatic Colon Cancer Cells. [Abstract]

2021 Mar 22;13(6):1438. PMID: 33809839
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
iScience

Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]

2024 May 16;27(6):110011. PMID: 38868181
Sci Rep

Epigenetic modulation through BET bromodomain inhibitors as a novel therapeutic strategy for progranulin-deficient frontotemporal dementia. [Abstract]

2024 Apr 20;14(1):9064. PMID: 38643236
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

dBET6 purchased from MedChemExpress. Usage Cited in: ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. [Abstract]

Immuno-blots of six cell lines, treated for 5 h with either DMSO or different concentrations of the degraders MZ1 and dBet6.
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
Noncoding RNA

Bromodomain and Extra-Terminal Family Proteins BRD2, BRD3, and BRD4 Contribute to H19-Dependent Transcriptional Regulation of Cell Adhesion Molecules, Modulating Metastatic Dissemination Program in Prostate Cancer. [Abstract]

2025 Apr 29;11(3):33. PMID: 40407591
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
Biosci Biotechnol Biochem

Synergistic effect of cerium chloride and calcium chloride alters calcium signaling in keratinocytes to promote epidermal differentiation. [Abstract]

2024 Nov 22;88(12):1432-1441. PMID: 39333009
University of Arizona

2026.
Res Sq

2026 Jun 23.
bioRxiv

Protein Age Bias in Target Degradation by PROTACs. [Abstract]

2026 May 5:2026.05.01.722262. PMID: 42146509
bioRxiv

Design and Development of DNA Damage Chemical Inducers of Proximity (DD-CIP) for Targeted Cancer Therapy. [Abstract]

2025 Nov 4:2025.11.03.686423. PMID: 41278667
bioRxiv

Development of Degraders and 2-pyridinecarboxyaldehyde (2-PCA) as a recruitment Ligand for FBXO22. [Abstract]

2025 Aug 20:2025.08.19.671158. PMID: 40894587
bioRxiv

2025 Jun 19.
bioRxiv

2025 April 16.
Patent

US20250041303A1.
bioRxiv

2024 September 26.
bioRxiv

Discovery of electrophilic degraders that exploit SNAr chemistry. [Abstract]

2024 Sep 27:2024.09.25.615094. PMID: 39386645
bioRxiv

Resistance of estrogen receptor function to BET bromodomain inhibition is mediated by transcriptional coactivator cooperativity. [Abstract]

2024 Jul 26:2024.07.25.605008. PMID: 39211208
bioRxiv

Exploration of the Tunability of BRD4 Degradation by DCAF16 Trans-labelling Covalent Glues. [Abstract]

2023 Oct 10:2023.10.07.561308. PMID: 37873358
Harvard University

2023 Mar. 30487357.
bioRxiv

Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. [Abstract]

2023 Feb 15:2023.02.14.528208. PMID: 36824856
Research Square Print

November 18th, 2022

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (59.43 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

1.1885 mL

5.9427 mL

11.8854 mL

5 mM

0.2377 mL

1.1885 mL

2.3771 mL

10 mM

0.1189 mL

0.5943 mL

1.1885 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (2.97 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (2.97 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

Protokoll

Animal Administration^[1]

Mice^[1]
MOLT4 human T-ALL cells are intravenously injected into NSG mice (2×10⁶ cells/mouse). Luminescence is utilized to monitor engraftment (evident at day 6), at which point mice are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 8), JQ1 (20 mg/kg QD, n = 9) or vehicle (captisol, n = 9) treatment for 14 days. Survival of all three cohorts is subsequently monitored using hind limb paralysis caused by high femoral leukemic burden as a defined endpoint. SUPT11 human T-ALL cells (mCherry⁺ and Luciferase⁺) are intravenously injected into NSG mice (2.52×10⁶ cells/mouse). Luminescence is used to monitor successful engraftment, occurring 10 days after injection. At this point, animals are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 7), JQ1 (7.5 mg/kg BID, n = 7) or vehicle (captisol, n = 7) treatment for 18 days. Treatment burden is assessed via total body luminescence imaging as well as by bone marrow infiltration by mCherry⁺ T-ALL cells^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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]. Winter GE, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell. 2017 Jul 6;67(1):5-18.e19. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1885 mL	5.9427 mL	11.8854 mL	29.7134 mL
	5 mM	0.2377 mL	1.1885 mL	2.3771 mL	5.9427 mL
	10 mM	0.1189 mL	0.5943 mL	1.1885 mL	2.9713 mL
	15 mM	0.0792 mL	0.3962 mL	0.7924 mL	1.9809 mL
	20 mM	0.0594 mL	0.2971 mL	0.5943 mL	1.4857 mL
	25 mM	0.0475 mL	0.2377 mL	0.4754 mL	1.1885 mL
	30 mM	0.0396 mL	0.1981 mL	0.3962 mL	0.9904 mL
	40 mM	0.0297 mL	0.1486 mL	0.2971 mL	0.7428 mL
	50 mM	0.0238 mL	0.1189 mL	0.2377 mL	0.5943 mL

Keywords

dBET6

40 Cited Publications

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dBET6

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) dBET6

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (40)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dBET6

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) dBET6

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (40)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dBET6 Related Classifications

HY-112588 Related Classifications