2. Epigenetics
  3. Epigenetic Reader Domain
  4. BET-IN-13

BET-IN-13 是一种有效的 BET 抑制剂，IC50 值为 1.6 nM。BET-IN-13 降低 LPS 诱导的 TNF-α、IL-1β、IL-6 和 NOS2 mRNA 表达水平。BET-IN-13 具有抗炎活性。BET-IN-13 具有研究急性肝损伤的潜力。

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BET-IN-13 Chemical Structure

BET-IN-13 Chemical Structure

CAS No. : 2506823-08-9

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BET-IN-13 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

BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury[1].

IC50 & Target[1]

BRD4 BD1

57.4 nM (IC50)

BRD4 BD2

44.4 nM (IC50)

BRD2 BD1

79.3 nM (IC50)

BRD2 BD2

27.5 nM (IC50)

BRD3 BD1

45.6 nM (IC50)

BRD3 BD2

18.9 nM (IC50)

BRDT BD1

87.0 nM (IC50)

BRDT BD2

43.4 nM (IC50)

体外研究
(In Vitro)

BET-IN-13 (compound 28) (1.1, 3.3, 10 µM, 2+6 h) 降低 RAW264.7 细胞中 LPS (500 ng/ml) 诱导的 TNF-α、IL-1β、IL-6 和 NOS2 mRNA 的表达水平[1]。

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

BET-IN-13 相关抗体:

RT-PCR[1]

Cell Line: RAW264.7 cells
Concentration: 1.1, 3.3, 10 µM
Incubation Time: Pre-treated for 2 h before stimulating with LPS for 6 h
Result: Significantly reduced LPS (500 ng/ml) induced TNF-α, IL-1β, IL-6 and NOS2 mRNA expression levels in a dose-dependent manner.
体内研究
(In Vivo)

BET-IN-13 (3 mg/kg；静脉注射；一次) 在小鼠中显示出良好的药代动力学 (PK) 特性，T1/2 为 0.69 h，AUCINF-obs 为 609 h*ng/mL 和 Vss 为 1717 mL/kg[1]。
BET-IN-13 (37.5、75 mg/kg；腹腔注射；一次) 降低 LPS/D-GalN(d-gaiactosamine)诱导的急性肝衰竭 (ALF) 小鼠的炎症和肝损伤而无明显毒性[1]。

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

Animal Model: 20-22g, Female C57BL/6J mice (LPS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF))[1]
Dosage: 37.5, 75 mg/kg
Administration: I.p.; once
Result: Reduced inflammatory responses associated with LPS/GalN-induced acute liver failure with the survival rate increased significantly to 69.2% for37.5 mg/kg and to 84.6% for 75 mg/kg.
分子量

497.56

Formula

C28H23N3O4S
CAS 号
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

BET-IN-13 相关分类

  • 摩尔计算器

  • 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:

BET-IN-132506823-08-9Epigenetic Reader DomainRAW264.7 cellsanti-inflammatoryLPSTNF-αacute liver injuryInhibitorinhibitorinhibit

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