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dBET1

Cat. No. 6327 1 Citation Submit a Review Datasheet / COA / SDS
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Description: (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
Chemical Name: (6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-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 (1)
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for dBET1

dBET1 is a Degrader (PROTAC®) comprising BET bromodomain antagonist (+)-JQ1 (Cat. No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Depletes BET bromodomains in cancer cell lines in vitro (EC50 = 430 nM in breast cancer cells) and induces apoptosis. Delays tumor growth and downregulates MYC in mice bearing human AML xenografts. Antibody validated for Western Blot also available: NBP2-77359.

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 dBET1

M. Wt 785.27
Formula C38H37ClN8O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1799711-21-9
PubChem ID 91799313
InChI Key LKEGXJXRNBALBV-PMCHYTPCSA-N
Smiles CC1=NN=C2[C@@H](N=C(C3=CC=C(C=C3)Cl)C4=C(N12)SC(C)=C4C)CC(NCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O

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 dBET1

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 78.53 100

Preparing Stock Solutions for dBET1

The following data is based on the product molecular weight 785.27. 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 1.27 mL 6.37 mL 12.73 mL
5 mM 0.25 mL 1.27 mL 2.55 mL
10 mM 0.13 mL 0.64 mL 1.27 mL
50 mM 0.03 mL 0.13 mL 0.25 mL

Molarity Calculator

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Product Datasheets for dBET1

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for dBET1

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

Winter et al (2015) Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370

Wurz et al (2017) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579

If you know of a relevant reference for dBET1, please let us know.

View Related Products by Target

Keywords: dBET1, dBET1 supplier, Proteolysis, Targeting, Chimera, PROTAC, PROTACs, cereblon, E3, ubiquitin, ligase, bromodomain, BRD4, targeted, protein, degradation, tpd, active, degraders, degrades, Bromodomains, Bromodomain, (BRD), Degraders, 6327, Tocris Bioscience

1 Citation for dBET1

Citations are publications that use Tocris products. Selected citations for dBET1 include:

Hao et al (2020) Highly Parallel Quantification and Compartment Localization of Transcription Factors and Nuclear Proteins. Cell Rep 30 2463-2471.e5 PMID: 32101728

Do you know of a great paper that uses dBET1 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!

*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