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. Antibody validated for Western Blot also available: NBP2-77359.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
-
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
Product Datasheets
Reconstitution Calculator
Molarity Calculator
Citation for dBET1
The citations listed below are publications that use Tocris products. Selected citations for dBET1 include:
1 Citation: Showing 1 - 1
-
Highly Parallel Quantification and Compartment Localization of Transcription Factors and Nuclear Proteins.
Authors: Hao Et al.
Cell Rep 2020;30:2463-2471.e5
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for dBET1
There are currently no reviews for this product. Be the first to review dBET1 and earn rewards!
Have you used dBET1?
Submit a review and receive an Amazon gift card.
$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
