dBET6

For research use only.

Catalog No.S8762

dBET6 Chemical Structure

Molecular Weight(MW): 841.37

dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.

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Biological Activity

Description dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.
Targets
BRD4 [1]
()
14 nM
In vitro

dBET6 is a highly cell-permeable degrader of BET bromodomains. It is potent in most cancer cell lines. dBET6 features highly increased cellular potency with evident degradation in the sub-nanomolar range. Treatment with 100 nM dBET6 leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis. dBET6 disrupts global productive transcription elongation. dBET6 treatment leads to a widespread decrease in steady-state mRNA levels, but observed an incommensurate impact on expression of members of the core regulatory circuitry of leukemogenic transcription factors. The collapse of the core transcriptional machinery prompted by BET degradation precedes a robust apoptotic response, of apparent translational significance[1].

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 29764999     


Relative cell viability of patient-derived gliomaspheres treated with the indicated concentrations of dBET6 for 5 d. IC50 values (mean, n = 3) of dBET6 are shown. 

29764999
Western blot
BRD2 / BRD3 / BRD4 / Aurora A / Aurora B / PLK1 / Cyclin B1 / p21 / E2F1 ; 

PubMed: 29764999     


Levels of cell cycle-related proteins in gliomaspheres after dBET6 treatment (50 nM, 24 h). 

p-RNA-Pol2 S2 / p-RNA-Pol2 S5 / RNA-Pol2 ; 

PubMed: 29764999     


Effect of dBET6 treatment on RNA-Pol2 phosphorylation. U87 and U251 GBM cells were incubated with dBET6 (0.5 µM and 1 µM, respectively) for indicated durations. 

29764999
In vivo

dBET6 is well tolerated. Upon dBET6 treatment, a significant reduction of leukemic burden is observed in a disseminated mouse model of T-ALL. Moreover, mice treated with dBET6 (7.5 mg/kg BID) exhibits a significant survival benefit compared to mice treated with vehicle control or JQ1 (20 mg/kg QD)[1].

Protocol

Cell Research:

[1]

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  • Cell lines: MOLT4 cells deficient in CRBN expression
  • Concentrations: 0.05, 0.1, 0.5, 1 μM
  • Incubation Time: 3 hr
  • Method:

    MOLT4 cells deficient in CRBN expression are treated with various concentrations of either dBET1 or dBET6 for 3 hr. Cells are collected by centrifugation, washed once with PBS and transferred into PCR tubes, spun down and incubated at 47.5°C for 3 min. After a subsequent incubation for 3 min on 25°C, cells are lysed by addition of 30 µL lysis buffer and three repeated freeze-thaw cycles using liquid nitrogen.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male CD-1 mice
  • Dosages: 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (118.85 mM)
Ethanol 42 mg/mL (49.91 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 841.37
Formula

C42H45ClN8O7S

CAS No. 1950634-92-0
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C)C2=C(S1)[N]3C(=NN=C3C(CC(=O)NCCCCCCCCNC(=O)COC4=CC=CC5=C4C(=O)N(C6CCC(=O)NC6=O)C5=O)N=C2C7=CC=C(Cl)C=C7)C

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID