PROTAC BRD4 Degrader-17

Names

[ CAS No. ]:
2585561-49-3

[ Name ]:
PROTAC BRD4 Degrader-17

Biological Activity

[Description]:

PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> PROTAC >> PROTAC
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4 (BD2):3.82 ± 0.0 nM (IC50)

BRD4 (BD1):29.54 ± 2. nM (IC50)


[In Vitro]

PROTAC BRD4 Degrader-17 (compound 13i) (100 nM，4-24 h) 在MV-4-11细胞中 4 h以 100 nM 的浓度显着诱导 BRD4 L 和 BRD4 S 降解，然后像 dBET6 一样在 24 h 恢复 BRD4 S[1]。

[References]

[1]. Chen J, et al. Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold. Eur J Med Chem. 2022 Jun 5;236:114259.  

Chemical & Physical Properties

[ Molecular Formula ]:
C49H47N7O9

[ Molecular Weight ]:
877.94

Related Compounds

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