1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. PROTAC BRD4 Degrader-8

PROTAC BRD4 Degrader-8 

Cat. No.: HY-138555 Purity: 97.04%
Handling Instructions

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.

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

PROTAC BRD4 Degrader-8 Chemical Structure

PROTAC BRD4 Degrader-8 Chemical Structure

Size Price Stock Quantity
1 mg USD 580 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].

IC50 & Target

IC50: 1.1 nM (BRD4 BD1), 1.4 nM (BRD4 BD2)[1]

In Vitro

PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].
PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].
PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC50 of 7.5 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1102.23

Formula

C₅₃H₆₁F₂N₉O₁₁S₂

SMILES

O[[email protected]](C[[email protected]]1C(NCC2=CC=C(C=C2)C3=C(N=CS3)C)=O)CN1C([[email protected]@H](NC(COCCOCCOCCNC(C4=CC(N(C5=NC=C(F)C=C5F)CC6=CNC7=C6C8=CN(C)C7=O)=C8C=C4CS(=O)(C)=O)=O)=O)C(C)(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 90 mg/mL (81.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9073 mL 4.5363 mL 9.0725 mL
5 mM 0.1815 mL 0.9073 mL 1.8145 mL
10 mM 0.0907 mL 0.4536 mL 0.9073 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: ≥ 4.5 mg/mL (4.08 mM); Clear solution

  • 2.

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

    Solubility: ≥ 4.5 mg/mL (4.08 mM); Clear solution

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

PROTAC BRD4 Degrader-8PROTACEpigenetic Reader DomainProteolysis-targeting chimeraBD1BD2PC3prostatecancerInhibitorinhibitorinhibit

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Product Name:
PROTAC BRD4 Degrader-8
Cat. No.:
HY-138555
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