2585561-49-3

2585561-49-3 structure

Name: PROTAC BRD4 Degrader-17
Chemical Name: PROTAC BRD4 Degrader-17
CAS Number: 2585561-49-3
Molecular Formula: C₄₉H₄₇N₇O₉
Molecular Weight: 877.94
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2023-05-31 20:35:12
Modify Date: 2024-01-31 23:19:21
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].

Name	PROTAC BRD4 Degrader-17

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.

Molecular Formula	C₄₉H₄₇N₇O₉
Molecular Weight	877.94