BRD4 Inhibitor-15

Names

[ CAS No. ]:
2761366-60-1

[ Name ]:
BRD4 Inhibitor-15

Biological Activity

[Description]:

BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Bcl-2 Family
Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Apoptosis >> Caspase
Signaling Pathways >> Apoptosis >> c-Myc
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4(1):18 ± 1.1 nM (IC50)

Bcl-2

Bax

Caspase-3

Procaspase-3


[In Vitro]

BRD4 Inhibitor-15 (compound 13) shows potent anti-proliferative activity against enzalutamide-resistant 22RV1 cells and LNCap cells, with IC50 values of 8.27 ± 0.28 and 7.33 ± 0.49 μM, respectively[1].

[References]

[1]. Jiang W, et al. Design, synthesis, and evaluation of novel pyridone derivatives as potent BRD4 inhibitors for the potential treatment of prostate cancer. Bioorg Chem. 2022 Feb;119:105575.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H21N3O2

[ Molecular Weight ]:
359.42

Related Compounds