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200626-61-5

中文名稱 1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE
英文名稱 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 2024/12/15 19:35:21
200626-61-5 結(jié)構(gòu)式 200626-61-5 結(jié)構(gòu)式

基本信息

中文別名
化合物ITSA1
英文別名
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)-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)119-121°C
儲存條件Inert atmosphere,2-8°C
溶解度二甲基亞砜:28mg/mL
形態(tài)固體
顏色白色至灰白色

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22
WGK Germany3

常見問題列表

生物活性
ITSA-1 是 HDAC 的激活劑,可抵消曲古抑菌素 A (trichostatin A, TSA) 誘導(dǎo)的細(xì)胞周期停滯,組蛋白乙?;娃D(zhuǎn)錄水平。
靶點(diǎn)

HDAC

體外研究

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.
體內(nèi)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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