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
- 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
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。
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靶点
HDAC
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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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