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Description: Potent and selective (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
Chemical Name: (6S)-4-(4-Chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥98% (HPLC)
Literature (4)

Biological Activity for dBET6

dBET6 is a potent and selective Degrader (PROTAC®) of BET bromodomains (IC50 = ~10 nM). dBET6 comprises BET antagonist (+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines through BRD4 degradation. Induces apoptosis. Reduces leukemic burden in a mouse model of T-ALL. Cell permeable.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for dBET6

E3 ligase CRBN
DC50 / Dmax 6 nM / 97% - Degradation of BRD4 in HEK293T cells after 3 h treatment
Kd (Degrader to Target) 46 nM - Kd of BRD4 BD1 was assessed by FP
Selectivity confirmed by global proteomics Yes
M. Wt 841.38
Formula C42H45ClN8O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1950634-92-0
PubChem ID 121427831
Smiles CC1=NN=C2[C@H](CC(=O)NCCCCCCCCNC(=O)COC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)N=C(C3=C(SC(C)=C3C)N12)C1=CC=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for dBET6

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 84.14 100

Preparing Stock Solutions for dBET6

The following data is based on the product molecular weight 841.38. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.19 mL 5.94 mL 11.89 mL
5 mM 0.24 mL 1.19 mL 2.38 mL
10 mM 0.12 mL 0.59 mL 1.19 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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References for dBET6

References are publications that support the biological activity of the product.

Winter et al (2017) BET Bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol. Cell 67 5 PMID: 28673542

Verstovsek et al (2017) Targeting cistrome and dysregulated transcriptome of post-MPN sAML. Oncotarget 8 93301 PMID: 29212143

Nowak et al (2018) Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat.Chem.Biol. 14 706 PMID: 29892083

If you know of a relevant reference for dBET6, please let us know.

Keywords: dBET6, dBET6 supplier, Potent, selective, active, degraders, degrades, BET, bromodomains, BRD4, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, degradation, JQ1, cell, permeable, in, vivo, tpd, Protein, Degraders, Bromodomains, 6945, Tocris Bioscience

Citations for dBET6

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Currently there are no citations for dBET6. Do you know of a great paper that uses dBET6 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia