SB-284851-BT

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].

Product Specifications

CAS Number

[219769-23-0]

UNSPSC

12352005

Target

Epigenetic Reader Domain; p38 MAPK

Type

Reference compound

Related Pathways

Epigenetics; MAPK/ERK Pathway

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/sb-284851-bt.html

Solubility

10 mM in DMSO

Smiles

FC1=CC=C(C2=C(C3=NC(OC4=CC(C)=CC(C)=C4)=NC=C3)N(C5CCNCC5)C=N2)C=C1

Molecular Formula

C26H26FN5O

Molecular Weight

443.52

References & Citations

[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.