AT 1
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%
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
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
-
Structural basis of PROTAC cooperative recognition for selective protein degradation.
Gadd et al.
Nat.Chem.Biol., 2017;
Product Datasheets
Reconstitution Calculator
Molarity Calculator
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for AT 1
Average Rating: 5 (Based on 1 Review)
Have you used AT 1?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Filter by:
We tested the effect of AT1 PROTAC in degrading the endogenous BRD4 protein in glioblastoma cell lines with varying concentrations of AT1 starting from 100nM, 300nM and 1 uM.