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
Biological ActivityAT 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
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.
Structural basis of PROTAC cooperative recognition for selective protein degradation.
Gadd et al.
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
Engineered PROTAC-CID systems for mammalian inducible gene regulation.
Authors: Ma Et al.
J Am Chem Soc 2023;145:1593
Chemo-proteomics exploration of HDAC degradability by small molecule degraders.
Authors: Eric S Et al.
Cell Chem Biol 2021;28:1514-1527.e4
Time-dependent effect of 1,6-hexanediol on biomolecular condensates and 3D chromatin organization.
Authors: Lin Et al.
Genome Biol 2021;22:230
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