價(jià)格 | ¥248 | ¥588 | ¥948 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱:化合物 ZL0420 | 英文名稱:ZL0420 |
CAS:2229039-45-4 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 97.77% | 產(chǎn)品類別: 抑制劑 |
貨號: T6828 |
名稱 | ZL0420 |
描述 | ZL0420 is a potent and selective bromodomain-containing protein 4 ( BRD4 ) inhibitor with nanomolar binding affinities to bromodomains (BDs) of BRD4. ZL0420 has IC 50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. |
動物實(shí)驗(yàn) | Male C57BL6/J mice housed under pathogen-free conditions with food and water ad libitum.?C57BL/6 mice were pre-treated in the absence or presence of the indicated BRD4 inhibitors [10 mg/kg body weight, via the intraperitoneal route] one day prior to poly stimulation.?The next day, animals were given another dose of BRD4 inhibitor immediately followed by intranasal ?administration of phosphate-buffered saline (PBS, 50 μL) or poly (300 μg dissolved in 50 μL PBS).?One day later, the mice were euthanized.?The bronchoalveolar lavage fluid (BALF) and lung tissues of treated mice were collected for further analysis.?Compounds were first dissolved in DMSO and further diluted in 10% hydroxypropyl β-cyclodextrin in PBS to appropriate concentration prior to intraperitoneal administration. |
體外活性 | ZL0420有效地結(jié)合到BRD4的乙酰化賴氨酸(KAc)結(jié)合口袋中,形成關(guān)鍵相互作用,包括通過一分子H2O間接與Tyr97建立的關(guān)鍵氫鍵和直接與Asn140的關(guān)鍵氫鍵。ZL0420在抑制TLR3依賴的天然免疫基因程序方面展現(xiàn)出亞μM級別的效力,這包括在培養(yǎng)的人類小氣道上皮細(xì)胞(hSAECs)中抑制ISG54、ISG56、IL-8和Groβ基因,IC50值為0.49-0.86μM[1]。 |
體內(nèi)活性 | ZL0420在低毒性條件下顯著有效降低小鼠模型的氣道炎癥。ZL0420具有高度的效力,幾乎完全阻斷了由poly(I:C)給藥引起的中小型氣道周圍中性粒細(xì)胞的大量積聚[1]。 |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 59 mg/mL (199.11 mM) |
關(guān)鍵字 | ZL 0420 | inhibit | Epigenetic Reader Domain | (E/Z)-ZL0420 | BRD4 | ZL0420 | airway inflammation | immune response genes | ZL-0420 | BET | bromodomains | Inhibitor |
相關(guān)產(chǎn)品 | Bisdemethoxycurcumin | dBET6 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | CeMMEC1 | (+)-JQ-1 | Curcumin | Naphthol AS-E | J-147 | ABBV-744 | Piflufolastat | Hexamethylene bisacetamide | Anacardic Acid |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 組蛋白修飾化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 表觀遺傳庫 | PPI抑制劑庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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