219769-23-0
Chemical Structure
SB-284851-BT
- CAS No.: 219769-23-0
- Formula:C26H26FN5O
- Molecular Weight:443.52
IUPAC Name: 2-(3,5-dimethylphenoxy)-4-(4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl)pyrimidine
InChIKey: UVLWMBRFRAMDOW-UHFFFAOYSA-N
SMILES: FC1=CC=C(C2=C(C3=NC(OC4=CC(C)=CC(C)=C4)=NC=C3)N(C5CCNCC5)C=N2)C=C1
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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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). | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
