1. Epigenetics
    PROTAC
  2. Epigenetic Reader Domain
    PROTAC
  3. BRD4 degrader AT1

BRD4 degrader AT1 

Cat. No.: HY-111433 Purity: 98.76%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 631 In-stock
Estimated Time of Arrival: December 31
5 mg USD 340 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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.

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].

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (102.81 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.17 mg/mL (1.20 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.17 mg/mL (1.20 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.17 mg/mL (1.20 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.76%

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BRD4 degrader AT1
Cat. No.:
HY-111433
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