2. Epigenetics Metabolic Enzyme/Protease Apoptosis
  3. Epigenetic Reader Domain Phosphatase c-Myc Apoptosis
  4. BRD4-IN-11

BRD4-IN-11 是一种口服有效的选择性的 BRD4 抑制剂 (IC50 = 26.35 nM (BD1)，IC50 = 72.81 nM (BD2))。BRD4-IN-11 对 BRD4 的效力比对 BRD2、BRD3 和 BRDT 的效力高出约 3 至 18 倍。BRD4-IN-11 增强 H2S 释放，抑制纤维化标志物 (α-SMA 和纤连蛋白)、c-Myc 和 CDC25B 的上调。BRD4-IN-11 减少 LO2 肝细胞中的细胞凋亡 (apoptosis)。BRD4-IN-11 在肝肺纤维化模型中可显著改善肝功能和肺功能，可用于研究肝肺纤维化。

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BRD4-IN-11

BRD4-IN-11 Chemical Structure

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BRD4-IN-11 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis[1].

IC50 & Target[1]

BRD4 (BD1)

26.35 nM (IC50)

BRD4 (BD2)

72.81 nM (IC50)

体外研究
(In Vitro)

BRD4-IN-11 (Compound 11r) 对 LX-2 细胞有抑制作用[1]。

BRD4-IN-11 (0.5-2.0 μM，48 小时) 可降低 Carbon tetrachloride (CCl4) (HY-Y0298) 处理的 LO2 细胞的凋亡率，抑制 CDC25B、α-SMA、c-Myc 和纤连蛋白的表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BRD4-IN-11 相关抗体:
体内研究
(In Vivo)

BRD4-IN-11 (Compound 11r) (15-30 mg/kg，口服，每日一次，3 天) 通过双重机制预防肝损伤和纤维化：在 CCl4 诱导的小鼠肝损伤模型中，抑制肝细胞凋亡和纤维化蛋白表达[1]。

BRD4-IN-11 (15-30 mg/kg，口服，每日一次，15 天) 可在 Bleomycin (BLM) (HY-108345) 诱导的肺纤维化 (PF) 模型中预防肺纤维化[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CCl4-induced (1 mg/kg, i.p.) male C57BL/6J mice (6-7weeks old) hepatic fibrosis model[1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: p.o., once a day, 3 days
Result: Alleviated CCl4-induced liver fibrosis, reduced collagen deposition in liver tissue and the increased expression of fibrosis biomarkers (type I collagen and α-SMA) in CCl4-treated mice, and alleviated CCl4-induced massive hepatocyte apoptosis.
Reduced liver weight coefficient and AST, ALT and TG levels at 30 mg/kg.
Had a safer and more effective ameliorative effect on CCl4-induced organ toxicity than JQ-1 (HY-78695), and that high dose is more effective than low dose.
Animal Model: BLM-induced (2 mg/kg, injected into the trachea) male C57BL/6J mice (6-7weeks old) PF model[1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: p.o., once a day, 15 days
Result: Reduced lung coefficient (lung weight/body weight ratio) and hydroxyproline content (a specific marker of collagen deposition and fibrosis severity), indicating effective attenuation of fibrosis at the molecular level.
Reduced inflammatory cell infiltration, decreased collagen deposition in lung tissue, and suppressed the expression of key fibrosis markers (i.e., collagen I and α-SMA) in BLM-injured lung tissue.
分子量

785.39

Formula

C40H37ClN4O5S3
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.
纯度 & 产品资料
参考文献

BRD4-IN-11 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD4-IN-11Epigenetic Reader DomainPhosphatasec-MycApoptosisMycInhibitorLX-2 cellsLO2 cellsCCl4-induced murine liver injure modelBLM induced PF modelinhibitorinhibit

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