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BRD4-IN-11 is an orally active and selective inhibitor of BRD4 with an IC50 of 26.35 nM for BD1 and 72.81 nM for BD2. Its potency against BRD4 is approximately 3 to 18 times greater than against BRr2, BRD3, and BRDT. BRD4-IN-11 increases H2S release and inhibits the upregulation of fibrosis markers (α-SMA and fibronectin), c-Myc, and CDC25B. It also reduces apoptosis in LO2 hepatic cells. In liver and lung fibrosis models, BRD4-IN-11 significantly improves liver and lung function, making it suitable for research on liver and lung fibrosis.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | BRD4-IN-11 is an orally active and selective inhibitor of BRD4 with an IC50 of 26.35 nM for BD1 and 72.81 nM for BD2. Its potency against BRD4 is approximately 3 to 18 times greater than against BRr2, BRD3, and BRDT. BRD4-IN-11 increases H2S release and inhibits the upregulation of fibrosis markers (α-SMA and fibronectin), c-Myc, and CDC25B. It also reduces apoptosis in LO2 hepatic cells. In liver and lung fibrosis models, BRD4-IN-11 significantly improves liver and lung function, making it suitable for research on liver and lung fibrosis. |
| Targets&IC50 | BRD4 BD1:26.35 nM |
| In vitro | BRD4-IN-11 (Compound 11r) demonstrates inhibitory effects on LX-2 cells. When applied at concentrations of 0.5-2.0 μM for 48 hours, BRD4-IN-11 reduces the apoptosis rate in LO2 cells treated with Carbon tetrachloride (CCl_4) and inhibits the expression of CDC25B, α-SMA, c-Myc, and fibronectin. |
| In vivo | BRD4-IN-11 (Compound 11r), administered orally at 15-30 mg/kg once daily for 3 days, serves to prevent liver injury and fibrosis via a dual mechanism: it inhibits hepatocyte apoptosis and fibrosis protein expression in a CCl4-induced mouse liver injury model. Additionally, BRD4-IN-11 given at the same dosage and frequency for 15 days can prevent pulmonary fibrosis in a Bleomycin (BLM)-induced lung fibrosis (PF) model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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