Name: BRD4-IN-11
Brand: TargetMol
SKU: T211473
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述	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.
靶点活性	BRD4 BD1:26.35 nM
体外活性	BRD4-IN-11 (Compound 11r) 对 LX-2 细胞表现出抑制活性。BRD4-IN-11 在 0.5-2.0 μM 浓度范围下，处理 LO2 细胞 48 小时，能降低 Carbon tetrachloride (CCl4) 引起的细胞凋亡率，并抑制 CDC25B、α-SMA、c-Myc 和纤连蛋白的表达。
体内活性	BRD4-IN-11 (Compound 11r) (15-30 mg/kg，口服，每日一次，3 天) 通过阻止 CCl4 诱导的小鼠肝损伤中肝细胞凋亡及抑制纤维化蛋白的表达来避免肝损伤和纤维化。BRD4-IN-11 (15-30 mg/kg，口服，每日一次，15 天) 在 Bleomycin (BLM) 诱导的肺纤维化 (PF) 模型中，可防止肺纤维化的发生。