ZL04203X 积分

目录号: GC19455纯度: >98.00%
A BRD4 inhibitor

ZL0420
Cas No.: 2230496-80-5
规格价格库存数量操作
5mg¥840.00现货
1
10mg¥1,260.00现货
1
25mg¥2,205.00现货
1
50mg¥3,290.00现货
1
10mM (in 1mL DMSO)¥924.00现货
1

文献被引

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产品描述 Description

ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

ZL0420 is well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H2O molecule. ZL0420 exhibits submicromolar potency of inhibiting the TLR3-dependent innate immune gene program, including ISG54, ISG56, IL-8, and Groβ genes in cultured human small airway epithelial cells (hSAECs) with IC50s of 0.49-0.86 µM[1].

ZL0420 demonstrates potent efficacy reducing airway inflammation in a mouse model with low toxicity. ZL0420 displays high efficacy and almost completely blocks the profound accumulation of neutrophils around the small and medium sized airways induced by poly(I:C) administration[1].

[1]. Liu Z, et al. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. Eur J Med Chem. 2018 May 10;151:450-461.

实验参考方法 Experimental Reference Method

Cell experiment:

hSAECs are first pretreated with a series final concentrations of BRD4 inhibitors from 0.01 nM to 100 µM for 24 hours and are then added poly(I:C) at 10 µg/mL for another 4 hours prior to harvesting the cells. The harvested cells are first ished with PBS twice and then the total RNA is extracted using acid guanidinium phenol extraction. The total RNA is further reverse-transcribed for gene expression analysis by Q-RT-PCR[1].

Animal experiment:

Mice[1]C57BL/6 mice are pre-treated in the absence or presence of the ZL0420 [10 mg/kg body weight, via the intraperitoneal route] one day prior to poly(I:C) stimulation. The next day, animals are given another dose of ZL0420 immediately followed by intranasal (i.n.) administration of phosphate-buffered saline (PBS, 50 µL) or poly(I:C) (300 µg dissolved in 50 µL PBS). One day later, the mice are euthanized. The bronchoalveolar lavage fluid (BALF) and lung tissues of treated mice are collected for further analysis[1].

References:

[1]. Liu Z, et al. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. Eur J Med Chem. 2018 May 10;151:450-461.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
2230496-80-5
SMILES
OC1=CC(N)=C(/N=N/C2=CC(CCC(N3)=O)=C3C=C2)C=C1C
分子式
C16H16N4O2
分子量
296.32 g/mol
溶解性
DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol