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200626-61-5

中文名称 1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE
英文名称 BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE
CAS 200626-61-5
分子式 C13H7Cl2N3O
分子量 292.12
MOL 文件 200626-61-5.mol
更新日期 2024/05/07 11:50:05
200626-61-5 结构式 200626-61-5 结构式

基本信息

中文别名
化合物ITSA1
英文别名
CS-2249
ITSA-1(ITSA1)
IFLAB-BB F0451-3184
1-(2,4-Dichlorobenzoyl)-1H-benzotriazole
BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE
Methanone, 1H-benzotriazol-1-yl(2,4-dichlorophenyl)-
所属类别
生物化工:激动剂抑制剂

物理化学性质

熔点119-121°C
储存条件Inert atmosphere,2-8°C
溶解度二甲基亚砜:28mg/mL
形态固体
颜色白色至灰白色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
危险品标志Xn
危险类别码22
WGK Germany3

常见问题列表

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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