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dBET6 | Degrader (PROTAC) of BRD4
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BRD4
  • IC50:14 nM BRD4
  • DC50:10-50 nM
Degrader (PROTAC)
50-100 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
BromoScan
Selectivity Assessment Description:
dBET6 is high selective for binding to BETs over other human bromodomains, as determined by singl ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Expression proteomics in MOLT4 cells

Potency
Cellular
In Vitro

BRD4

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1073/pnas.1712363115

In Vivo Validations

Mouse
Dose: 10 mg/Kg, Reviewers suggest: 7.5 mg/Kg BID
Route of delivery: Intraperitoneal
Plasma half life: 0.87 h

DOI Reference: 10.1073/pnas.1712363115

Orthogonal Probes def

MZ1
AT1
MS436

Chemical Information

Molecular Formula C42H45ClN8O7S
SMILEs Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)NCCCCCCCCNC(=O)COc1cccc3c1C(=O)N(C1CCC(=O)NC1=O)C3=O)c1nnc(C)n1-2
InChI InChI=1S/C42H45ClN8O7S/c1-23-24(2)59-42-35(23)37(26-13-15-27(43)16-14-26)46-29(38-49-48-25(3)50(38)42)21-33(53)44-19-8-6-4-5-7-9-20-45-34(54)22-58-31-12-10-11-28-36(31)41(57)51(40(28)56)30-17-18-32(52)47-39(30)55/h10-16,29-30H,4-9,17-22H2,1-3H3,(H,44,53)(H,45,54)(H,47,52,55)/t29-,30?/m0/s1
Molecular weight 840.28 Da
AlogP 5.24286
HBond acceptors 15
HBond donors 3
Atoms 104

References

Publications

Cross References

canSARChEMBL

Vendors

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Expert Reviews

by SERP
(on 18 Dec 2020 )
Cellular Use Rating
In Model Organisms
dBET6 is a cell-permeable chemical cereblon-based degrader of BET bromodomain protein (nanomolar degradation of BRD4, BRD3 and BRD2). dBET6 was well tolerated in 2-weeks mouse in vivo xenograpf model...
by SERP
(on 7 Jan 2021 )
Cellular Use Rating
In Model Organisms
dBET6 is a high-quality and mouse in vivo capable chemical probe for the proteasomal mediated degradation of BRD2, BRD3 and BRD4. Due to the use of a cereblon binder, any phenotypic effects observed...
by SERP
(on 7 Jan 2021 )
Cellular Use Rating
In Model Organisms
High quality probe which has been characterized extensively in vitro and in vivo with demonstrated target engagement via CETSA. Improved cellular potency and target engagement over another BRD4 PROTAC...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria