AT 1

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AT 1 | CAS No. 2098836-45-2 | Active Degraders
1 Image
Description: (+)-JQ1 based PROTAC® with selectivity for BRD4

Chemical Name: (2S,4R)-1-(2R)-2-Acetamido-3-[[6-[2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamido]hexyl]thio]-3-methylbutanoyl]-4-hydroxy-N-[4-(4-methylthiazol-5-yl)benzyl)pyrrolidinine-2-carboxamide

Purity: ≥98%

Product Details
Citations (3)

Biological Activity

AT 1 is a cell penetrant Proteolysis Targeting Chimera (PROTAC®) compound based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. Rationally designed based on a ternary complex crystal structure to improve selectivity for BRD4 degradation compared to MZ1 (Cat.No. 6154). Demonstrates profound and selective degradation of BRD4 in cells at 1-3 μM, with negligible loss of BRD2 and BRD3.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license

Technical Data

Soluble to 100 mM in DMSO and to 100 mM in ethanol
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.

Additional Information

Licensing Caveats:
Sold under licence from the University of Dundee

Product Datasheets

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Citations for AT 1

The citations listed below are publications that use Tocris products. Selected citations for AT 1 include:

3 Citations: Showing 1 - 3


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