1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. dBET1

dBET1 

Cat. No.: HY-101838 Purity: 99.24%
Handling Instructions

dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to Thalidomide (HY-14658) with a linker.

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

dBET1 Chemical Structure

dBET1 Chemical Structure

CAS No. : 1799711-21-9

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to Thalidomide (HY-14658) with a linker[1].

IC50 & Target

BRD4

430 nM (EC50)

Cereblon

 

In Vitro

Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50= 0.14 μM, compare to IC50= 1.1 μM with JQ1)[1].

In Vivo

Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count[1].

Molecular Weight

785.27

Formula

C₃₈H₃₇ClN₈O₇S

CAS No.

1799711-21-9

SMILES

O=C(NCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[[email protected]]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 43.33 mg/mL (55.18 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2734 mL 6.3672 mL 12.7345 mL
5 mM 0.2547 mL 1.2734 mL 2.5469 mL
10 mM 0.1273 mL 0.6367 mL 1.2734 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

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

Purity: 99.24%

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Keywords:

dBET1dBET 1dBET-1PROTACEpigenetic Reader DomainProteolysis-targeting chimeraInhibitorinhibitorinhibit

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Product name:
dBET1
Cat. No.:
HY-101838
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