AT 1

Modify Date: 2024-01-14 16:39:17

AT 1 Structure
AT 1 structure
Common Name AT 1
CAS Number 2098836-45-2 Molecular Weight 972.68
Density N/A Boiling Point N/A
Molecular Formula C48H58ClN9O5S3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AT 1


BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

 Names

Name BRD4 degrader AT1

 AT 1 Biological Activity

Description BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
Related Catalog
Target

Kd: 44 nM (Brd4BD2, cell assay), 38.8 nM (Brd4BD2 QVK, cell assay), 111 nM (Brd2BD1, cell assay), 94 nM (Brd2BD2, cell assay), 35 nM (Brd3BD1, cell assay), 39 nM (Brd3BD2, cell assay), 75 nM (Brd4BD1, cell assay), 35 nM (Brd2BD1 KEA, cell assay)[1]

In Vitro BRD4 degrader AT1 is a highly selective Brd4 degrader, with a Kd of 44 nM, for Brd4BD2 in cells. BRD4 degrader AT1 also shows Kds of 38.8 nM for a mutant Brd4BD2 (QVK), 111 ± 14 nM for Brd2BD1, 94 ± 9 nM for Brd2BD2, 35 ± 3 nM for Brd3BD1, 39 ± 8 nM for Brd3BD2, 75 ± 23 nM for Brd4BD1 and 35 ± 4 nM for a Brd2BD1 mutant (KEA). BRD4 degrader AT1 (1-3 μM) causes remarkable Brd4-selective depletion and has no or little activity against Brd2 and Brd3[1].
References

[1]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.

 Chemical & Physical Properties

Molecular Formula C48H58ClN9O5S3
Molecular Weight 972.68
Storage condition 2-8℃
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