1. Epigenetics
    PROTAC
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    PROTAC

BRD4 degrader AT1 

Cat. No.: HY-111433
Handling Instructions

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

For research use only. We do not sell to patients.

BRD4 degrader AT1 Chemical Structure

BRD4 degrader AT1 Chemical Structure

CAS No. : 2098836-45-2

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5 mg USD 340 Get quote
10 mg USD 590 Get quote
25 mg USD 1200 Get quote
50 mg USD 2100 Get quote

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0281 mL 5.1404 mL 10.2809 mL
5 mM 0.2056 mL 1.0281 mL 2.0562 mL
10 mM 0.1028 mL 0.5140 mL 1.0281 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

972.68

Formula

C₄₈H₅₈ClN₉O₅S₃

CAS No.

2098836-45-2

SMILES

CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[[email protected]@H](CC(NCCCCCCSC(C)(C)[[email protected]](NC(C)=O)C(N4[[email protected]@H](C[[email protected]@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)C7=NN=C(C)N27

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BRD4 degrader AT1
Cat. No.:
HY-111433
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BRD4 degrader AT1

Cat. No.: HY-111433