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dTRIM24 | dTRIM24 : Degrader (PROTAC) of TRIM24
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
TRIM24
  • IC50:338 nM
  • Dmax:72-76 %
Degrader (PROTAC)
2.5 to 5 uM
5 uM

Selectivity

In Vitro Selectivity Assessment

Potency: KD - BRD1 130 nM, BRPF1 52 nM

Potency Assay Off-Target:
BromoScan
Selectivity Assessment Description:
dTRIM24 in vitro binding assay to panel of human bromodomain proteins by single-point screening at 1 ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Outside target family: Proteomics analysis of MCF-7 cells

Potency
Cellular
In Vitro

TRIM24

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-018-0010-y

Negative Control Compounds

eTRIM24

Chemical Information

Molecular Formula C55H68N8O13S2
SMILEs CCCOc1cccc(Oc2cc3c(cc2NS(=O)(=O)c2cccc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)c2)n(C)c(=O)n3C)c1
InChI InChI=1S/C55H68N8O13S2/c1-8-20-75-40-12-10-13-41(28-40)76-47-30-45-44(61(6)54(69)62(45)7)29-43(47)60-78(70,71)42-14-9-11-38(26-42)51(66)56-19-21-72-22-23-73-24-25-74-33-48(65)59-50(55(3,4)5)53(68)63-32-39(64)27-46(63)52(67)57-31-36-15-17-37(18-16-36)49-35(2)58-34-77-49/h9-18,26,28-30,34,39,46,50,60,64H,8,19-25,27,31-33H2,1-7H3,(H,56,66)(H,57,67)(H,59,65)/t39-,46+,50-/m1/s1
Molecular weight 1112.43 Da
AlogP 0.0
HBond acceptors 21
HBond donors 5
Atoms 146

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 9 Feb 2021 )
Cellular Use Rating
dTRIM24 is a high-quality targeted degrader of TRIM24. It has been subjected to many of the best-available TPD validation experiments where it shows: potent and elective biochemical target engagement...
by SERP
(on 18 Feb 2021 )
Cellular Use Rating
dTRIM24 is a potent and selective PROTAC molecule targeting TRIM24, which has been suggested as a dependency in numerous cancers. The dTRIM24 is formed by the conjugation of the TRIM24 ligand IACS-7e...
by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
( The reviewer did not leave any comments )
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