| Identification | Back Directory | [Name]
Pyrimidine, 2-(3,5-dimethylphenoxy)-4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]- | [CAS]
219769-23-0 | [Synonyms]
Pyrimidine, 2-(3,5-dimethylphenoxy)-4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]- | [Molecular Formula]
C26H26FN5O | [MOL File]
219769-23-0.mol | [Molecular Weight]
443.52 |
| Hazard Information | Back Directory | [Uses]
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]. | [Definition]
ChEBI: SB-284851-BT is a piperidinylimidazole that is 1H-imidazole carrying a piperidin-4-yl group, 4-fluorophenyl group and a 2-(3,5-dimethylphenoxy)pyrimidin-4-yl group at positions 1, 4 and 5 respectively. It is a potent inhibitor of p38alpha mitogen-activated protein kinase and BRD4. It has a role as a bromodomain-containing protein 4 inhibitor and an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor. It is a member of monofluorobenzenes, an aryloxypyrimidine and a piperidinylimidazole. | [IC 50]
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. DOI:10.1021/acs.jmedchem.8b01248
[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. DOI:10.1016/j.drudis.2021.08.007 |
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