Home / Product Type / PROTAC® Degraders & Targeted Protein Degradation / Protein Degraders / Bromodomain (BRD) Degraders / dBET6

dBET6

Cat. No. 6945 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

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
InChI Key JGQPZPLJOBHHBK-UFXYQILXSA-N
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
Solubility
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.

View Related Products by Target

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, Bromodomains, Bromodomain, (BRD), Degraders, 6945, Tocris Bioscience

Citations for dBET6

Citations are publications that use Tocris products.

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

Reviews for dBET6

There are currently no reviews for this product. Be the first to review dBET6 and earn rewards!

Have you used dBET6?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
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