PROTAC BRD4 Degrader-17

Modify Date: 2024-01-31 23:19:21

PROTAC BRD4 Degrader-17 Structure
PROTAC BRD4 Degrader-17 structure
Common Name PROTAC BRD4 Degrader-17
CAS Number 2585561-49-3 Molecular Weight 877.94
Density N/A Boiling Point N/A
Molecular Formula C49H47N7O9 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PROTAC BRD4 Degrader-17


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].

 Names

Name PROTAC BRD4 Degrader-17

 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
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
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