生物活性 靶点 体外研究 体内研究
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ChemicalBook  CAS数据库列表  1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE

1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE

生物活性 靶点 体外研究 体内研究
1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE,200626-61-5,结构式
1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE
  • CAS号:200626-61-5
  • 英文名:BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE
  • 中文名:1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE
  • CBNumber:CB4697730
  • 分子式:C13H7Cl2N3O
  • 分子量:292.12
  • MOL File:200626-61-5.mol
1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE化学性质
  • 熔点 :119-121°C
  • 储存条件 :Inert atmosphere,2-8°C
  • 溶解度 :DMSO: ~28mg/mL
  • 形态 :solid
  • 颜色 :White to Off-White
安全信息
  • 危险品标志 :Xn
  • 危险类别码 :22
  • WGK Germany :3

1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE性质、用途与生产工艺

  • 生物活性 ITSA-1 是 HDAC 的激活剂，可抵消曲古抑菌素 A (trichostatin A, TSA) 诱导的细胞周期停滞，组蛋白乙酰化和转录水平。
  • 靶点

    HDAC

  • 体外研究

    ITSA1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA1 is also able to effect cell cycle rescue over longer duration.
    ITSA1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells.
    ITSA1 (50 μM; 2 hours; A549 and murine ES cells cells) treatment suppresses TSA-induced histone acetylation. Importantly, suppression of acetylation levels is only observable when ITSA1 is added concurrent with or post TSA treatment.
    ITSA1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells.

    Cell Cycle Analysis

    Cell Line: Murine ES cells
    Concentration: 50 μM
    Incubation Time:
    Result: Served to revert the TSA-arrested population to a normal cell cycle distribution.

    Apoptosis Analysis

    Cell Line: A549 cells
    Concentration: 50 μM
    Incubation Time: 5 hours
    Result: Reduced the number of apoptosis.

    Western Blot Analysis

    Cell Line: A549 and murine ES cells
    Concentration: 50 μM
    Incubation Time: 2 hours
    Result: Reduced histone acetylation to the baseline level.

    RT-PCR

    Cell Line: Murine ES cells
    Concentration: 50 μM
    Incubation Time: 30 minutes
    Result: Suppressed TSA-activated transcription.
  • 体内研究

    ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS +/− mice) treatment balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling.

    Animal Model: CBS +/− mice
    Dosage: 0.5 mg/kg
    Administration: Intraperitoneal injection; 3 times/week; for 8 weeks
    Result: Balanced deacetylation activity and suppressed IL-6 and TNF-α expression.
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