BRD4 Inhibitor-20

Research use only, not for human use.

BRD4 Inhibitor-20 is a potent bromodomain protein 4 (BRD4) inhibitor with oral activity, demonstrating antiproliferative effects in cancer cell lines and used in studies of various cancers, including colon cancer.

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.

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).BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc.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.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 phaseWestern Blot Analysis Cell Line:HT-29 cells Concentration:0.5, 2.5, 5.0 μM Incubation Time:24 h Result: Displayed profound inhibitory effects on c-Myc protein expression.Cell Proliferation Assay Cell Line:HT-29, HL-60 and WI-38 cells Concentration:Incubation Time:72 h Result:Possessed strong anti-proliferative activity and weak toxicity.Cell Cycle Analysis Cell Line:HT-29 cell lines Concentration:2.5, 5.0, 10.0 μM Incubation Time:24 h Result:Arrested the cell-cycle progression of the cell line into the G1 phases and the percentage of cells in G1 phase after treatment under concentrations of 2.5, 5.0 and 10.0 μM were 85.98%, 86.49% and 86.05%, respectively.

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie.

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Chromatin/Epigenetic

Epigenetic Reader Domain

Epigenetic Reader Domain

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2490311-14-1

358.41

C18H18N2O4S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (348.76 mM; Ultrasonic (<60°C)

C(C)(C)=C1C=2C(NC1=O)=CC=C(NS(=O)(=O)C3=C(OC)C=CC=C3)C2

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(-20℃)

With Ice Pack

≥ 2 years