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PROTAC® comprising BET 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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under license from Dana-Farber Cancer Institute.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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.
|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|
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
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Keywords: dBET1, dBET1 supplier, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, BRD4, degradation, Ubiquitin, Ligases, Active, Degraders, Bromodomains, 6327, Tocris Bioscience
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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* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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
- Degrader Building Blocks
- Custom Degrader Services
- UPS Proteins and Assays
- Assays for Protein Degradation
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
Adapted from the 2015 Cancer Product Guide Edition 3, 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
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