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BRD4 degrader AT1

Catalog No. T5439 CAS 2098836-45-2

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

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BRD4 degrader AT1, CAS 2098836-45-2

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5 mg	4-5 weeks	$ 1,100.00

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Biological Description

Chemical Properties

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Description	BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
Targets&IC50	BRD2 BD1 KEA:35 nM (Kd), BRD3 BD1:35 nM (Kd), BRD2 BD2:94 nM (Kd), BRD4 BD1:75 nM (Kd), BRD4 BD2:44 nM (Kd), BRD3 BD2:39 nM (Kd), BRD4 BD2QVK:38.8 nM (Kd), BRD2 BD1:111 nM (Kd)
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].

Molecular Weight	972.68
Formula	C48H58ClN9O5S3
CAS No.	2098836-45-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 201. May;13(5):514-521.

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Keywords

BRD4 degrader AT1 2098836-45-2 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor inhibit PROTACs BRD-4 degrader AT1 inhibitor

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