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AT 1

Catalog #: 6356
3 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6356/5
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)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

M.Wt:
972.68
Formula:
C48H58ClN9O5S3
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2098836-45-2

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

Reconstitution Calculator
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Reconstitution Calculator

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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

  1. Engineered PROTAC-CID systems for mammalian inducible gene regulation.
    Authors: Ma Et al.
    J Am Chem Soc  2023;145:1593
  2. Chemo-proteomics exploration of HDAC degradability by small molecule degraders.
    Authors: Eric S Et al.
    Cell Chem Biol  2021;28:1514-1527.e4
  3. 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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