dBET6
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).
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 1950634-92-0
- Formula: C42H45ClN8O7S
- Molecular Weight:841.37
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) dBET6
More- Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
- Mol Cell. 2021 Sep 2;81(17):3589-3603.e13. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2024 Jul 2;15(1):5379. [Abstract]
- Nat Commun. 2024 Jun 26;15(1):5409. [Abstract]
- Nat Commun. 2024 Mar 11;15(1):2192. [Abstract]
- Nat Chem Biol. 2024 Dec;20(12):1640-1649. [Abstract]
- Nat Chem Biol. 2023 Dec;19(12):1513-1523. [Abstract]
- Nat Chem Biol. 2023 Mar;19(3):323-333. [Abstract]
- Blood Cancer Discov. 2026 Jul 1;7(4):624-641. [Abstract]
- Cell Rep Med. 2025 Dec 16;6(12):102467. [Abstract]
- Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
- Cell Genom. 2024 Sep 4:100651. [Abstract]
- NPJ Precis Oncol. 2023 Feb 18;7(1):20. [Abstract]
- J Med Chem. 2026 May 28;69(10):12669-12677. [Abstract]
- J Med Chem. 2026 Mar 19. [Abstract]
- Cancers (Basel). 2021 Mar 22;13(6):1438. [Abstract]
- Structure. 2024 Dec 5;32(12):2352-2363.e8. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- Sci Rep. 2024 Apr 20;14(1):9064. [Abstract]
- ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. [Abstract]
- J Immunol. 2021 Jul 15;207(2):493-504. [Abstract]
- Noncoding RNA. 2025 Apr 29;11(3):33. [Abstract]
- Biochem Biophys Res Commun. 2022 Nov 5:628:68-75. [Abstract]
- Biosci Biotechnol Biochem. 2024 Nov 22;88(12):1432-1441. [Abstract]
- University of Arizona. 2026.
- Res Sq. 2026 Jun 23.
- bioRxiv. 2026 May 5:2026.05.01.722262. [Abstract]
- bioRxiv. 2025 Nov 4:2025.11.03.686423. [Abstract]
- bioRxiv. 2025 Aug 20:2025.08.19.671158. [Abstract]
- bioRxiv. 2025 Jun 19.
- bioRxiv. 2025 April 16.
- Patent. US20250041303A1.
- bioRxiv. 2024 September 26.
- bioRxiv. 2024 Sep 27:2024.09.25.615094. [Abstract]
- bioRxiv. 2024 Jul 26:2024.07.25.605008. [Abstract]
- bioRxiv. 2023 Oct 10:2023.10.07.561308. [Abstract]
- Harvard University. 2023 Mar. 30487357.
- bioRxiv. 2023 Feb 15:2023.02.14.528208. [Abstract]
- Research Square Print. November 18th, 2022
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Bio/Physico-chemical Assay
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WB
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Flow Cytometry
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WB
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Cell Proliferation/Viability Assay
All PROTACs Isoforms
More
Biological Activity
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BET |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
10.33 nM
Compound: dBET6
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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
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[PMID: 35395439] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1950634-92-0
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Appearance Solid
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Molecular Weight 841.37
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Formula C42H45ClN8O7S
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Color White to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (40)
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Journal Impact Factor
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Most Recent
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Nat Immunol
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.
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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
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 CRL4CRBN-based degrader dBET6.
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Nat Commun
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
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 BRD4BD2-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).
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Nat Chem Biol
2023 Dec;19(12):1513-1523. PMID: 37653169 -
Nat Chem Biol
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).
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Blood Cancer Discov
2026 Jul 1;7(4):624-641. PMID: 42149820 -
Cell Rep Med
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
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.
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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 -
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bioRxiv
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 -
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bioRxiv
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 -
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bioRxiv
Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. [Abstract]2023 Feb 15:2023.02.14.528208. PMID: 36824856 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
Purity & Documentation
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Data Sheet (276 KB)
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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)
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Handling Instructions (2659 KB)
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, 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 |