BRD4 Inhibitor-20

• CAT Number: I042920
• CAS Number: 2490311-14-1
• Molecular Formula: C18H18N2O4S
• Molecular Weight: 358.41
• Purity: ≥95%
• Synonyms: 2-methoxy-N-(2-oxo-3-propan-2-ylidene-1H-indol-5-yl)benzenesulfonamide
• InChI: InChI=1S/C18H18N2O4S/c1-11(2)17-13-10-12(8-9-14(13)19-18(17)21)20-25(22,23)16-7-5-4-6-15(16)24-3/h4-10,20H,1-3H3,(H,19,21)
• InChIKey: CDERLIUJSXSXFH-UHFFFAOYSA-N
• SMILES: CC(=C1C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=CC=C3OC)NC1=O)C

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer[1].
BRD4 Inhibitor-20 (compound 12j) exhibits excellent BRD4 inhibitory activities (BD1, IC50=19 nM; BD2, IC50=28 nM) and inhibitory activities against BRD2 (BD1, IC50=24 nM; BD2, IC50=18 nM)[1].
BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc[1].
BRD4 Inhibitor-20 (72 h) has anti-proliferation potency with IC50 values of 4.75 μM, 1.35 μM and 44.07 μM in HT-29, HL-60 and WI-38 cells, respectively[1].
BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase[1].
BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie[1].

Reference

[1]. Yu Xu, et al. Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. Eur J Med Chem. 2020 Dec 15;208:112780.
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