BRD4 Inhibitor-20 是一种有效的溴结构域蛋白 4 (BRD4) 抑制剂，具有口服活性。 BRD4 Inhibitor-20 对 BRD4 (BD1) 和BRD4 (BD2) 具有抑制活性，IC50值分别为 19 nM 和 28 nM。 BRD4 Inhibitor-20 在癌细胞系中也具有抗增殖活性。 BRD4 Inhibitor-20 可用于结肠癌等多种癌症的研究。
| 生物活性 | BRD4Inhibitor-20 is a potent orally activebromodomain protein 4 (BRD4)inhibitor.BRD4Inhibitor-20 has inhibitory activity forBRD4(BD1) andBRD4(BD2) withIC50values of 19 nM and 28 nM, respectively.BRD4Inhibitor-20 also has anti-proliferation activities incancercell lines.BRD4Inhibitor-20 can be used for the research of kinds ofcancer, such as coloncancer[1]. |
| IC50& Target[1] | BRD4 BD1 19 nM (IC50) | BRD4 BD2 28 nM (IC50) | BRD2 (BD1) 24 nM (IC50) | BRD2 (BD2) 18 nM (IC50) |
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体外研究
(In Vitro) | 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 IC50values 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].
Western Blot Analysis[1] | 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[1] | 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[1] | 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. |
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体内研究
(In Vivo) | BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie[1].
| Animal Model: | rats[1] | | Dosage: | 5 mg/kg, 15 mg/kg | | Administration: | intravenous dosing (iv) or oral dosing (po) | | Result: | | PK Parameters | iv (5 mg/kg) | po (15 mg/kg) | | Cmax(μg/L) | - | 2175 | | Tmax(h) | - | 1.00 | | t1/2(h) | 1.56 | 3.59 | | CLz/F (L/h/kg) | 0.68 | 1.03 | | AUC0–t(μg/L*h) | 7296 | 14384 | | AUC0–∞(μg/L*h) | 7340 | 14600 | | F (%) | - | 66% | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
