SB-284851-BT

Names

[ CAS No. ]:
219769-23-0

[ Name ]:
SB-284851-BT

Biological Activity

[Description]:

SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET)[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

p38α:0.47 nM (Kd)

BRD4-BD1:1.7 μM (IC50)

BRDT (1):18 μM (IC50)

BRD4(1):3.7 μM (IC50)


[References]

[1]. Divakaran A, et al. Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. J Med Chem. 2018 Oct 25;61(20):9316-9334.  

[2]. Jin W, et al. Dual-target inhibitors of bromodomain-containing protein 4 (BRD4) in cancer therapy: Current situation and future directions. Drug Discov Today. 2022 Jan;27(1):246-256.  

Chemical & Physical Properties

[ Molecular Formula ]:
C26H26FN5O

[ Molecular Weight ]:
443.52

Related Compounds