1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE
| 中文名稱(chēng) | 1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE |
|---|---|
| 中文同義詞 | 化合物ITSA1;(1H-苯并[D][1,2,3]三唑-1-基)(2,4-二氯苯基)甲酮;ITSA-1,HDAC激活劑;ITSA-1,HDAC活化劑;化合物ITSA1,10 MM DMSO 溶液;ITSA-1激活劑 |
| 英文名稱(chēng) | BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE |
| 英文同義詞 | IFLAB-BB F0451-3184;BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE;1-(2,4-Dichlorobenzoyl)-1H-benzotriazole;ITSA-1(ITSA1);CS-2249;Methanone, 1H-benzotriazol-1-yl(2,4-dichlorophenyl)-;(1H-Benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone;inhibit,Histone deacetylases,ITSA-1,Inhibitor,HDAC,ITSA 1 |
| CAS號(hào) | 200626-61-5 |
| 分子式 | C13H7Cl2N3O |
| 分子量 | 292.12 |
| EINECS號(hào) | |
| 相關(guān)類(lèi)別 | 活性小分子庫(kù);標(biāo)準(zhǔn)品 |
| Mol文件 | 200626-61-5.mol |
| 結(jié)構(gòu)式 |  |
1-(2,4-DICHLOROBENZOYL)-1H-BENZOTRIAZOLE 性質(zhì)
| 熔點(diǎn) | 119-121°C |
|---|---|
| 儲(chǔ)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 | 白色至類(lèi)白色 |
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HDAC
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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. |
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. |