dBET1
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%
Biological Activity
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.PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data
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.
Additional Information
Background References
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A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation.
Wurz et al.
J.Med.Chem., 2018;61:453 -
Drug development. Phthalimide conjugation as a strategy for in vivo target protein degradation.
Winter et al.
Science, 2015;348:1376
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Citation for dBET1
The citations listed below are publications that use Tocris products. Selected citations for dBET1 include:
1 Citation: Showing 1 - 1
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Highly Parallel Quantification and Compartment Localization of Transcription Factors and Nuclear Proteins.
Authors: Hao Et al.
Cell Rep 2020;30:2463-2471.e5
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